- A chemoenzymatic scalable route to optically active (R)-1-(pyridin-3-yl)-2- aminoethanol, valuable moiety of β3-adrenergic receptor agonists
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Enantiomerically pure (R)-2-chloro-1-(pyridin-3-yl)ethanol has been prepared by kinetic resolution performed in the presence of Candida antarctica SP435-L lipase immobilized on a macroporous polyacrylate resin (Novozym 435). It was converted into (R)-1-(pyridin-3-yl)-2-aminoethanol, left-hand side of β3-adrenergic receptor ligands.
- Perrone, Maria Grazia,Santandrea, Ernesto,Giorgio, Erika,Bleve, Laura,Scilimati, Antonio,Tortorella, Paolo
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- NOVEL SULFONAMIDE SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA-3 ADRENORECEPTOR AGONISTS
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This invention relates to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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Page/Page column 27
(2008/12/07)
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- Solvent and in situ catalyst preparation impacts upon Noyori reductions of aryl-chloromethyl ketones: application to syntheses of chiral 2-amino-1-aryl-ethanols
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As part of medicinal chemistry efforts we found it necessary to develop general syntheses of highly enantiomerically enriched 1-aryl-2-chloroethanols and 1-aryl-2-methylaminoethanols. A survey of literature methods suggested that a truly general approach had not yet been reported, encouraging us to undertake the development of such a methodology. This study describes the design, development, and reduction to practice of a general synthesis of chiral 1-aryl-2-chloroethanols and the transformation of these entities to highly enantiomerically enriched 1-aryl-2-methylaminoethanols. Of particular importance were observations of the impact of solvent and the method of catalyst preparation on the yield and enantiomerical excess of chlorohydrins prepared via Noyori transfer hydrogenations of aryl-chloromethyl ketones.
- Tanis, Steven P.,Evans, Bruce R.,Nieman, James A.,Parker, Timothy T.,Taylor, Wendy D.,Heasley, Steven E.,Herrinton, Paul M.,Perrault, William R.,Hohler, Richard A.,Dolak, Lester A.,Hester, Matthew R.,Seest, Eric P.
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p. 2154 - 2182
(2007/10/03)
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- INDOLE, INDAZOLE, AND BENZAZOLE DERIVATIVE
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The compound of the formula (I): wherein W is a group of the following formula (VIII) binding to any possible position on the Q: Q is, together with W, a group of the formula: -C(M=C(R3A)-N(R3)-, etc.; R3A is H or optionally substituted lower alkyl; R4, R5, R6, and R7 are independently H or optionally substituted lower alkyl; R1 is optionally substituted lower alkyl, etc.; R2 is H, etc.; R3 is H, etc.; Ar is phenyl, etc., or a pharmaceutically acceptable salt thereof, where these compounds exhibiting β3-adrenoceptor-stimulating activity and being useful as a medicament for treatment of obesity, etc.
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Page/Page column 20
(2010/02/11)
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- A practical synthesis of optically active aromatic epoxides via asymmetric transfer hydrogenation of α-chlorinated ketones with chiral rhodium-diamine catalyst
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A practical method for the synthesis of optically active aromatic epoxides has been developed via the formation of optically active α-chlorinated alcohols and intramolecular etherification. Optically active alcohols with up to 99% ee can be obtained from
- Hamada, Takayuki,Torii, Takayoshi,Izawa, Kunisuke,Ikariya, Takao
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p. 7411 - 7417
(2007/10/03)
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- PROCESS TO PRODUCE ENANTIOMERICALLY ENRICHED 1-ARYL- AND 1-HETEROARYL-2-AMINOETHANOLS
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The invention relates to a method of preparing enantiomerically enriched amino alcohols of Formula (I) wherein the variable R1, R2, and R3 are defined herein.
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- 2,6-Substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
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This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
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- Carboxyl substituted chroman derivatives useful as beta 3 adrenoreceptor agonists
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This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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- CARBOXYL SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA 3 ADRENORECEPTOR AGONISTS
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This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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- SULFONAMIDE SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA 3 ADRENORECEPTOR AGONISTS
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This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
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- SUBSTITUTED SULFONAMIDES AS SELECTIVE BETA-3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY
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Substituted sulfonamides are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent
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- SUBSTITUTED SULFONAMIDES AS SELECTIVE BETA3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY
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Substituted sulfonamides are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent
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