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A novel 4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivative or a pharmaceutically acceptable salt thereof, which is useful as an agent for treating or preventing nocturia and/or diabetes insipidus, is provided.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A convenient and efficient route for the enantioselective synthesis of functionalised beta-hydroxy N-acetylcysteamine thioesters is described. The route allows the facile incorporation of vicinal 13C labelling to produce intermediates required for biosynthetic studies on a wide range of polyketide metabolites, e.g. 6-MSA, monocerin, colletodiol and strobilurins.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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The first example of a regioselective beta-arylation of benzo[b]thiophenes and thiophenes at room temperature with aryl iodides as coupling partners is reported. This methodology stands out for its operational simplicity: no prefunctionalization of either starting material is required, the reaction is insensitive to air and moisture, and it proceeds at room temperature. The mild conditions afford wide functional group tolerance, often with complete regioselectivity and high yields, resulting in a highly efficient catalytic system. Initial mechanistic studies, including 13C and 2H KIEs, suggest that this process occurs via a concerted carbo-palladation across the thiophene double bond, followed by a base-assisted anti-elimination.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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The catalytic asymmetric aza-Michael reaction of benzoyl hydrazine toward chalcones through the nonactivated amine moiety conjugated addition was facilitated by the developed N,N?-dioxide-Sc(OTf)3 complex under mild conditions, affording the pharmacologically and synthetically useful products in moderate to high yields with up to 97% ee. The Royal Society of Chemistry.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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A series of glycosylated diol and triol derivatives was synthesized in order to serve as model compounds for the analysis of the stereochemistry, regiochemistry, and defect structures of poly(vinyl glycoside)s. 13C NMR spectroscopic analysis of these compounds revealed that the attached chiral carbohydrate substituents induced a strong correlation of the chemical shifts of both the anomeric C and the alpha-C atom of the aglycon with the absolute configuration of the latter. The influence of the stereoconfiguration of beta- and gamma-C atoms as well as the regiochemistry of the aglycon on the chemical shifts of the alpha-C and the anomeric C atom was also investigated. Wiley-VCH Verlag GmbH & Co. KGaA, 2009.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Enantioselective epoxide hydrolysis by yeasts has been demonstrated for the hydrolysis of several aryl, alicyclic and aliphatic epoxides by a strain of Rhodotorula glutinis. High enantioselectivity was obtained in the hydrolysis of methyl substituted aryl and aliphatic epoxides whereas selectivity towards terminal epoxides in all cases was lower. Homochiral vicinal diols were formed from several methyl substituted epoxides and also from meso epoxides. Kinetic resolution of trans-1-phenyl-1,2-epoxypropane was studied in more detail.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Herein we report the synthesis of gamma-keto-delta-alkenyl-phosphonates and phosphine oxides by two versions of strategy (a) which involves the addition of dialkyl phosphites to alpha,alpha?-diarylideneketones, and by strategy (b) which utilizes the reaction of P-chlorodiphenylphosphine with diarylidene ketones in acetic acid. On reaction with hydrazine derivatives, gamma-keto-delta-alkenyl-phosphonates and phosphine oxides give 3-phosphonoethylpyrazoline derivatives which can be converted into the corresponding aromatic pyrazoles by oxidative dehydrogenation, using sodium nitrite as oxidizing agent.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Prostereogenic mono- and dicarbamates of 1,3-propanediol and 1,4-butanediol are deprotonated by the sec-butyllithium/(-)-sparteine system with high enantiotopic differentiation.The electrophilic substitution of the intermediate chiral carbanions furnishes the title compounds with >95percent ee. Key words: Chiral 1-oxy-carbanions; enantioselective deprotonation; (-)-sparteine.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Spiroannulation has been achieved by double Michael reaction under very mild conditions using a phase transfer catalyst.Various cyclohexanone molecules having different steric requirements have been condensed with 1,5-diphenyl-1,4-pentadien-3-one in the presence of cetyltrimethylammonium bromide.This condensation reaction was found to be diastereospecific as well as regiospecific.Stereoisomers derived from homotopic cycloalkanones were found to adopt endo geometry, while diastereotopic cycloalkanones were found to elaborate a mixture of endo and exo diastereomers.These stereochemical inferences are drawn based on extensive 2D-nmr studies employing COSY and NOESY experiments.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate