Category: 4254-15-3

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

To (S)-propane diol (4.89 g, 64.2 mmol) in DCM (20 ml_) at -20 0C (CO2/ ethylene glycol bath) was added TEA (11.2 ml_, 80.3 mmol) followed by p-toluenesulfonyl chloride (12.3 g, 64.3 mmol) in DCM (26 mL) dropwise over 30 minutes. The cold bath was allowed to expire while stirring for 26h. DCM was added and the reaction was washed with 1 N HCI, water, and brine. The organic layer was dried (MgSO4), filtered, and concentrated in vacuo. The residue was purified by silica gel chromatography (0-40% EtOAc/Hex over 40 minutes) to provide the tosylate (8.37 g, 36 .4 mmol).

As the paragraph descriping shows that 4254-15-3 is playing an increasingly important role.

Reference£º
Patent; SCHERING CORPORATION; WO2009/5645; (2009); A1;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

To a stirred solution of 68 (S)-2-propanediol (1.00g, 13.14mmol) in 14 dichloromethane/69 pyridine (10:10 V/V) at -25C under argon was added dropwise 70 p-toluenesulfonyl chloride (2.51g, 13.14mmol) dissolved in 10mL of CH2Cl2 over a period of 2h. The mixture was stirred at -25C for 4h and then at room temperature for further 2h. After the reaction was completed, 30mL of CH2Cl2 were added and the mixture was shaken successively with ice-cold water, 1M 10mL 71 aqueous HCl, 15mL 72 water, saturated NaHCO3, and water, respectively. The organic phase was dried over MgSO4 and filtered and the solvent was removed under reduced pressure. The residue was purified by chromatography over silica gel using toluene/EtOAc (5/1) to give 73 product (1.70g, 56%) as white crystals. M.p: 33-35C, [alpha]D25=-12.05 (c 1, CHCl3). 1H NMR (CDCI3, ppm): delta 7.80 (d, 2H, J=8.0Hz, of OTs), 7.36 (d, 2H, J=8.0Hz, of OTs), 3.97-4.05 (m, 2H, -CHCH3-+CH2OTs (a)), 3.83-3.88 (m, 1H, CH2OTs (b)), 2.45 (s, 3H, -CH3 of OTs), 2.39 (s, 1H, OH), 1.15 (d, J=6.4Hz, 3H, -CHCH3), assignment was based on the 1H-13C HETCOR and 1H-1H COSY spectra

The synthetic route of 4254-15-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Article; Meric, Nermin; Kayan, Cezmi; Guerbuez, Nevin; Karakaplan, Mehmet; Binbay, Nil Ertekin; Aydemir, Murat; Tetrahedron Asymmetry; vol. 28; 12; (2017); p. 1739 – 1749;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

To a stirred solution of (A)-propane-l,2-diol (5 g, 65.7 mmol) in anhydrous DCM (40 mL) at 0 C, was added imidazole (4.47 g, 65.7 mmol), followed by TBDMS-C1 (10.89 g, 72.3 mmol). After being stirred at room temperature for 4 h, the reaction mixture was cooled to 0C, and partitioned between sodium bicarbonate solution (50 ml) and DCM (200 mL). The organic layer was washed with EhO, and saturated NaCl solution, dried over anhydrous Na2S04, filtered and concentrated under reduced pressure fV)- l -((/tW-butyl dimethyl si lyl)oxy)propan-2-ol ^2 g, 63.0 mmol, 96% ) as colourless oil. NMR (400 MHz, chloroform-^ d ppm 3.73 – 3.88 (m, 1H), 3.51 – 3.65 (m, 1H), 3.29 – 3.46 (m, 1H), 2.36 – 2.56 (m, 1H), 1.12 (d, J=6.53 Hz, 3H), 0.90 – 0.96 (m, 9H), 0.06 – 0.13 (m, 6H).

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Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; BALOG, James Aaron; SEITZ, Steven P.; WILLIAMS, David K.; ANDAPPAN MURUGAIAH SUBBAIAH, Murugaiah; (191 pag.)WO2019/136112; (2019); A1;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

4254-15-3, (S)-Propane-1,2-diol is a chiral-oxygen-ligands compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

(1) Feeding800 kg of S-propylene glycol, 1600 kg of dimethyl carbonate and 8 kg of sodium methoxide solution were added to the reaction vessel, and heating and stirring were started.The sodium methoxide solution is a 30percent sodium methoxide/methanol solution;The S-propanediol has a propylene glycol content of 99.5percent, a moisture content of 0.5percent, and a specific rotation of ?16.80-17. (2) Temperature rise reactionFirst stage heating reaction The temperature is raised to 60-65 ¡ã C, at which time a solution (mainly methanol, a small portion of dimethyl carbonate) is distilled off, received in the receiving tank, and the solution is evaporated; Second stage heating reactionThereafter, after about 12 hours, the temperature is raised from 65 ¡ã C to 90 ¡ã C, the solution is kept distilled, and the product is distilled as a by-product alcohol-based fuel (methanol and dimethyl carbonate); Third stage temperature rise reactionHeating was continued, and the temperature was raised from 90 ¡ã C to 115 ¡ã C for 8 hours, and the heating was stopped. (3) Cooling downThe temperature was lowered from 115 ¡ã C to 60 ¡ã C. The temperature in the reaction vessel is ?90 ¡ã C, and the alcohol-based fuel (mixed solution of methanol and dimethyl carbonate) is distilled off; most of the steam distilled out at >90 ¡ã C is dimethyl carbonate, and a small amount of methanol is used as a reaction raw material for recovery. (4) Decompression reaction under reduced pressureStart decompression under reduced pressure, using vacuum distillation, vacuum degree ? -0.08mpa, the temperature rises at a rate of 0.2 ¡ã C per minute,Continue to distill the solution (a mixture of methanol and dimethyl carbonate),Keep the solution evaporated, when the temperature rises to 120 ¡ã C, basically no solvent comes out at this time,The pressure reduction and desolvation can be stopped, and the temperature is lowered; the remaining liquid in the reaction tank is (S)-propylene carbonate. In the crude (S)-propylene carbonate, the (S)-propylene carbonate content is 97percent or more. From the start of the preparation to the preparation of the crude product, the reaction time was 25 hours. (5) Distillation reactionTransfer the remaining liquid after decompression and decompression to the rectification bottle, and turn on the heating and stirring.Vacuuming, ensuring a vacuum degree ? 0.1Mpa, starting the steaming before the fraction, steaming out about 100kg of the former fraction, and then transferring the finished product.The materials in the rectification tank were all distilled off, the rectification was stopped, and (S)-propylene carbonate was collected. The (S)-propylene carbonate has the following quality indicators:1. Appearance: colorless clear liquid;2, SPC chemical purity content (percent): ? 99.8;3, SPC optical purity content (percent): ? 99.4;4. SPC isomer content (percent): ? 0.6;5. Moisture (percent): ? 0.1; The yield of the finished SPC is 97percent; the specific rotation is -2 to -3;

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Reference£º
Patent; Weifang Huitao Chemical Co., Ltd.; Liu Jianwei; Zhang Quansheng; Wei Lanxing; Hua Xian; (6 pag.)CN109369401; (2019); A;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

Example 29; N-r(2Z)-3-butviri.31thiazolor4.5-clpyridin-2(3H)-ylidenel-2-(r(2S)-2-hvdroxypropylloxyl-5 -(trifluoromethyl)benzamide; (S)-propane-l,2-diol (52 mg, 0.68 mmol) in THF (1 mL) was treated with NaH (60percent dispersion; 27 mg, 0.68 mmol) at room temperature for 20 minutes. The mixture was cooled to O0C and a solution of Example 2OB (90 mg, 0.23 mmol) in THF (1 mL) was added. The mixture was allowed to warm to room temperature, and stirred for 4 hours. The mixture was diluted with saturated aqueous NaHCO3 (20 mL) and extracted with ethyl acetate (2 x 30 mL). The combined organic extracts were dried over anhydrous Na2SO4, filtered, and concentrated. The residue was purified by column chromatography using an Analogix.(R). Intellifiash280 .(TM). (SiO2, 0-100 percent ethyl acetate in hexanes) to afford 19 mg (19percent) of the title compound. 1H NMR (500 MHz, CDCl3) delta ppm 1.04 (t, J=7.48 Hz, 3 H) 1.28 (d, J=6.41 Hz, 3 H) 1.47 – 1.59 (m, 2 H) 1.88 – 1.98 (m, 2 H) 3.87 (t, J=8.85 Hz, 1 H) 4.21 – 4.31 (m, 1 H) 4.35 (dd, J=9.15, 2.75 Hz, 1 H) 4.51 – 4.59 (m, 2 H) 7.12 (d, J=8.85 Hz, 1 H) 7.72 (dd, J=8.54, 2.14 Hz, 2 H) 8.51 (d, J=I.83 Hz, 2 H) 8.75 (s, 1 H); MS (DCI/NH3) m/z 454 (M+H)+.

As the paragraph descriping shows that 4254-15-3 is playing an increasingly important role.

Reference£º
Patent; ABBOTT LABORATORIES; FROST, Jennifer, M.; LATSHAW, Steven, P.; DART, Michael, J.; CARROLL, William, A.; PEREZ-MEDRANO, Arturo; KOLASA, Teodozyj; PATEL, Meena; NELSON, Derek, W.; LI, Tongmei; PEDDI, Sridhar; WANG, Xueqing; LUI, Bo; WO2010/71783; (2010); A1;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

4254-15-3, (S)-Propane-1,2-diol is a chiral-oxygen-ligands compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

To a yellow foamy solid 4 (131.77 g, 295.11 mmol) was added (S)-(+)-1,2-propanediol (296.0 ml) and purified water (866.0 ml).Stir and slowly cool after dissolving.Stirring crystallized, filtered and drained to give a crude product 5;The crude product 5 was directly recrystallized from methyl tert-butyl ether (900 ml) without drying.After filtering to get a fine 5;Without drying, recrystallize twice with methyl tert-butyl ether (900 ml) and filter.The filter cake is washed twice with methyl tert-butyl ether.After drying, it is dried in a drying oven at 45-50C.The second boutique 5 (116.37g, 231.22mmol),HPLC purity 99.94% [HPLC normalization method:Column Agilent SB-C18 (250¡Á4.6mm 5mum);The mobile phase is mobile phase A with acetonitrile-water-trifluoroacetic acid (30:70:0.025).The mobile phase B was acetonitrile-water-trifluoroacetic acid (90:10:0.025).Gradient elution (0?20 min: A 100%?70%, 20?40 min: A 70%?10%, 40?50 min: A 10%, 50?50.1 min:A 100%, 50.1 ? 60min: A 100%,) detection wavelength 220nm;Column temperature 30C; flow rate, 1.0 ml/min], yield 78.35%.

As the paragraph descriping shows that 4254-15-3 is playing an increasingly important role.

Reference£º
Patent; Shanghai Modern Pharmaceutical Co., Ltd.; Zhang Guang; Shen Gang; Zou Lingyan; Fu Min; Wu Miaomiao; (13 pag.)CN107488156; (2017); A;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

To separate the propylene glycol enantiomers on a chiral gas chromatography column, they were derivatized with acetic anhydride to the methyl esters. Into a small vial equipped with a Teflon lined stir bar was added 1 mL diethyl ether and equal amounts (5-10 drops) propylene glycol, pyridine, and acetic anhydride. The reaction mixture was stirred 3 hours at room temperature, washed with deionized 0 (3 x 1 mL) and dried over Na2S04. The derivatized product was then analyzed via gas chromatography. The diacetate was obtained with an ee of 97percent when (R,i?)-(Cl-salcy)CoN03 was used, and with an ee of 96percent when (5,S)-(Cl-salcy)CoN03 was used, indicating that both enantiomers produced highly regioregular poly(propylene succinate).

As the paragraph descriping shows that 4254-15-3 is playing an increasingly important role.

Reference£º
Patent; CORNELL UNIVERSITY; COATES, Geoffrey; WHITEHEAD, Julie; (60 pag.)WO2016/25675; (2016); A1;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

General procedure: A 45percent solution of hydrogen bromide in acetic acid (33.0 g, 23.2 mL) was added dropwise over 10 min to 60.3 mmol optically active diol 4a-f with stirring and ice-cooling. The solution was stirred at 0 ¡ãC for 5 min, and next at room temperature for 45 min. Next, water (100 mL) was added, and the mixture was alkalized to pH 8 with solid Na2CO3. The solution was immediately extracted with ethyl ether (5 .x. 60 mL), and the combined extracts were dried over anhydrous Na2SO4. The ether was evaporated, and the product was distilled under reduced pressure or purified by silica gel column chromatography with gradient AcOEt-hexane 9:1.

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Reference£º
Article; Poterala, Marcin; Plenkiewicz, Jan; Tetrahedron Asymmetry; vol. 22; 3; (2011); p. 294 – 299;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

Example 33 : (2R, 75R)-2-[(l-Aminoisoquinolin-6-yl)amino]-8-fluoro-7- {[(25)-l- hydroxypropan-2-yl]oxy } -4, 15,20-trimethyl- 13 -oxa-4, 1 1- diazatricyclo[14.2.2.16, 10]henicosa-l(18),6,8, 10(21), 16, 19-hexaene-3, 12-dione; trifluoroacetic acid [00356] To a solution of (s)-(+)-l,2-propanediol (2.0 g, 26.3 mmol) in DMF (5 mL) was added TBS-C1 (5.94 g, 39.4 mmol) and imidazole (2.147 g, 31.5 mmol). The reaction was stirred at 25 ¡ãC for 18 h. The reaction mixture was partitioned between ethyl acetate and sat. ammonium chloride. The organic phase was washed with sat. ammonium chloride and brine, dried (MgS04) and concentrated in vacuo. The crude product was purified by flash chromatography to give 33A (4.0 g, 80percent yield) as a colorless oil. 33B: (5)-Benzyl 2-((l-((tert-butyldimethylsilyl)oxy)propan-2-yl)oxy)-3-fluoro-5- nitrobenzyl(methyl)carbamate [00357] To a solution of 27B (400 mg, 1.197 mmol), 33A (251 mg, 1.316 mmol) and triphenylphosphine (345 mg, 1.316 mmol) in THF (10 mL) at 0 ¡ãC, was added DIAD (0.256 mL, 1.316 mmol) dropwise. The reaction mixture was allowed to slowly warm to rt and stirred for 16 h, then was concentrated. The crude product was purified by flash chromatography (0 to 40percent ethyl acetate/hexanes) to give 33B (577 mg, 1.139 mmol, 95percent yield) as colorless oil. MS (ESI) m/z: 507.1 [M+1]+. H MR (400 MHz, chloroform-d) delta ppm 7.78 – 7.94 (2 H, m) 7.27 – 7.43 (5 H, m) 5.17 (2 H, d, J=20.1 Hz) 4.46 – 4.74 (3 H, m) 3.65 – 3.81 (2 H, m) 2.97 (3 H, d, J=15.8 Hz) 1.31 (3 H, t, J=7.0 Hz) 0.81 (9 H, d, J=7.0 Hz) -0.05 – 0.04 (6 H, m) rotamers. 33C: (S)-4-((l-((tert-Butyldimethylsilyl)oxy)propan-2-yl)oxy)-3-fluoro-5- ((methylamino)methyl)aniline [00358] To a degassed solution of 33B (573 mg, 1.131 mmol) in MeOH (10 mL), was added 10percent Pd-C (50 mg, 0.047 mmol). The mixture was evacuated and flushed with H2 (3X), then was stirred under an atmosphere of H2 for 8 h. The mixture was filtered and concentrated to give 33C (382 mg, 1.115 mmol, 99percent yield) as a pale brown oil. MS (ESI) m/z: 343.1 [M+l]+. PI MR (400 MHz, chloroform-d) delta ppm 6.40 (1 H, d, J=1.8 Hz) 6.33 (1 H, dd, J=12.5, 2.8 Hz) 4.20 (1 H, sxt, J=5.7 Hz) 3.62 – 3.79 (4 H, m) 3.53 (2 H, br. s.) 2.40 (3 H, s) 1.25 (3 H, d, J=6.3 Hz) 0.89 (9 H, s) 0.05 (6 H, s). 33D: tert-Butyl N- {6-[({[(5-amino-2- { [(25)- l-[(tert-butyldimethylsilyl)oxy]propan-2- yl]oxy } -3 -fluorophenyl)methyl](methyl)carbamoyl} ( {4-[(2R)- 1 -hydroxypropan-2-yl]-3 – methylphenyl} )methyl)amino]isoquinolin- 1 -yl} -N-[(tert-butoxy)carbonyl]carbamate [00359] To Intermediate 5 (100 mg, 0.515 mmol), Intermediate 1 (185 mg, 0.515 mmol), and glyoxylic acid monohydrate (47.4 mg, 0.515 mmol), were added DMF (6.00 mL) and acetonitrile (6 mL). The mixture was stirred at 80 ¡ãC for 1 h, then was cooled to rt. To the mixture were added sequentially 33C (201 mg, 0.587 mmol), DMF (6.00 mL), TEA (0.215 mL, 1.546 mmol) and BOP (251 mg, 0.567 mmol). The reaction mixture was stirred at rt for 1 h, then was diluted with H20 and extracted with EtOAc (3X). The extract was washed with brine, dried ( a2S04) and concentrated. The crude product was purified by flash chromatography (1 to 15percent MeOH/methylene chloride) to give 33D (422 mg, 0.474 mmol, 92percent yield) as an orange foam. MS (ESI) m/z: 890.3 [M+l]+. H MR: complicated due to presence of diastereomers and amide rotamers. Example 33 [00360] To a solution of 33D (417 mg, 0.468 mmol) in dichloromethane (10 mL) and acetonitrile (5 mL) at 0 ¡ãC, was added phosgene (20percent in toluene, 0.243 mL, 0.492 mmol) dropwise. The mixture was stirred at 0 ¡ãC for 20 min, then was removed from the cooling bath and bubbled with Ar for 20 min. This mixture was added dropwise via a syringe pump into a solution of TEA (0.392 mL, 2.81 mmol) in dichloromethane (190 mL) over 5 h. The reaction mixture was allowed to stir at rt for 11 h, and then concentrated. The crude product was purified by flash chromatography (1 to 15percent MeOH/methylene chloride) to give a mixture of diastereoisomers. The diastereomers were separated by a prep chiral HPLC (R,R-Whelk-0 column 21.1 x 250 mm). The desired fractions were combined and concentrated. The residue was treated with TFA (4 mL) for 15 min. The reaction mixture was concentrated and purified by prep HPLC to give Example 33 (52.9 mg, 0.074 mmol, 31.4percent yield) white solid. MS (ESI) m/z: 602.2 [M+l]+. NMR (400 MHz, methanol-d4) delta ppm 8.05 (1 H, d, J=9.3 Hz) 7.64 (1 H, dd, J=7.8, 1.8 Hz) 7.44 (1 H, d, J=7.8 Hz) 7.31 (1 H, d, J=7.0 Hz) 7.18 – 7.23 (2 H, m) 6.91 (1 H, d, J=7.3 Hz) 6.83 (1 H, d, J=2.3 Hz) 6.53 (1 H, dd, J=12.4, 2.4 Hz) 5.73 (1 H, s) 5.66 (1 H, br. s.) 5.37 (1 H, d, J=17.1 Hz) 4.65 (1 H, t, J=11.0 Hz) 4.27 – 4.38 (1 H, m, J=5.7, 5.7, 5.7, 5.7, 5.4 Hz) 4.06 (1 H, d, J=17.3 Hz) 3.96 (1 H, dd, J=10.8, 4.3 Hz) 3.63 (2 H, d, J=4.8 Hz) 3.43 – 3.55 (1 H, m) 3.27 (3 H, s) 2.34 (3 H, s) 1.30 (3 H, d, J=7.0 Hz) 1.27 (3 H, d, J=6.3 Hz). Analytical HPLC (low pH, 254 nM): Sunfir…

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Reference£º
Patent; BRISTOL-MYERS SQUIBB COMPANY; ZHANG, Xiaojun; GLUNZ, Peter W.; PRIESTLEY, Eldon Scott; JOHNSON, James, A.; WURTZ, Nicholas, Ronald; LADZIATA, Vladimir; WO2013/184734; (2013); A1;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4254-15-3,(S)-Propane-1,2-diol,as a common compound, the synthetic route is as follows.

The four (4) step reaction sequence starting from 103-1 and 103-2 (prepared as shown from S-(+)-1,2-propanediol (103-0)) provided Boc-T103a in a very good overall yield of 85%. The alternatively protected analogue Ddz-T103a was prepared using the same procedure with an overall yield of 55% [1.4 g Ddz(2RMe)opy18 was obtained starting from 1 g (5.8 mmol) of 103-1]. Synthesis of the Boc-T103b stereoisomer proceeds similarly, but starting from R-(-)-1,2-propanediol.TLC: Rf: 0.3 (100% EtOAc)

The synthetic route of 4254-15-3 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; Tranzyme Pharma Inc.; US2008/194672; (2008); A1;,
Synthesis and Crystal Structure of a Chiral?C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis
Chiral lanthanide(III) complexes of sulphur¨Cnitrogen¨Coxygen ligand derived from aminothiourea and sodium?D-camphor-¦Â-sulfonate