Asymmetric synthesis of the cholesteryl ester transfer protein inhibitor torcetrapib
Previously our group reported synthetic efforts used to synthesize kilogram quantities of the cholesteryl ester transfer protein (CETP) inhibitor torcetrapib, 1, via a mid-stage resolution. This account describes research conducted to develop an asymmetri
Damon, David B.,Dugger, Robert W.,Hubbs, Stephen E.,Scott, Jill M.,Scott, Robert W.
p. 472 - 480
(2012/12/22)
Method for optical resolution of 3-aminopentanenitrile
Durch ein neues Verfahren zur Spaltung von racemischem 3-Aminopentannitril k?nnen enantiomerenangereichertes 3-Aminopentannitril oder dessen Salze gewonnen werden. Hierzu wird racemisches 3-Aminopentannitril mit einer enantiomerenangereicherten organischen S?ure umgesetzt, eines der beiden anfallenden diastereomeren Salze abgetrennt und anschlie?end in das enantiomerenangereicherte 3-Aminopentannitril oder dessen Salze überführt.
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Page 7
(2008/06/13)
PREPARATION OF CHIRAL AMINO-NITRILES
A process and intermediates for producing 3-amino nitrites. The process involves resolving an enantiomeric mixture of chiral 3-amino nitrites in the presence of a chiral acid in a solvent system to produce a chiral 3-amino nitrile salt. The process may fu
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Page 5
(2008/06/13)
BIOCATALYTIC PREPARATION OF ENANTIOMERICALLY ENRICHED AMINOPENTANENITRILE
Methods for preparing enantiomerically enriched aminopentanenitriles are provided. The methods involve selective acylation of an enantiomeric mixture of 3-aminopentanenitrile or selective hydrolysis of an enantiomeric mixture of 3-aminopentanenitrile amide in the presence of an enzyme selected from the group comprising lipase, esterase, and acylase. The methods yield R-aminopentanenitrile, which can be used to produce pharmaceutical products.
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Page 22
(2010/02/07)
Intermediates of CETP inhibitors
This invention relates to intermediates useful in the preparation of CETP inhibitors and methods of preparation thereof.
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(2008/06/13)
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