Invention Grant
US08278486B2 Process and intermediates for the preparation of N-acylated-4-aryl beta-amino acid derivatives
有权
用于制备N-酰化-4-芳基β-氨基酸衍生物的方法和中间体
- Patent Title: Process and intermediates for the preparation of N-acylated-4-aryl beta-amino acid derivatives
- Patent Title (中): 用于制备N-酰化-4-芳基β-氨基酸衍生物的方法和中间体
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Application No.: US12650128Application Date: 2009-12-30
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Publication No.: US08278486B2Publication Date: 2012-10-02
- Inventor: Shulin Wu , Bo Yu , Yejing Wang , Alain Delice , Jingyang Zhu
- Applicant: Shulin Wu , Bo Yu , Yejing Wang , Alain Delice , Jingyang Zhu
- Applicant Address: US NJ Monmouth Junction
- Assignee: Chiral Quest, Inc.
- Current Assignee: Chiral Quest, Inc.
- Current Assignee Address: US NJ Monmouth Junction
- Agency: Fox Rothschild LLP
- Agent Peter J. Butch, III; Robert N. Henrie, II
- Main IPC: C07C239/00
- IPC: C07C239/00

Abstract:
A process for producing an enantiomerically enriched compound of Formula I: where the R-configuration, or S-configuration at the stereogenic center is marked with an *; by hydrogenating an enamide of formula III: in an organic solvent in the presence of a catalyst comprising a transition metal selected from rhodium or iridium, complexed to a chiral diphosphine ligand; Ar is optionally substituted phenyl; Z is OR1, SR1 or NR1R2; and P is R3, OR3 or NR3R4; R1 and R2 are selected from H, C1-8 alkyl, C5-12 cycloalkyl, aryl and aryl-C1-2-alkyl; or R1 and R2 together with the nitrogen atom form a C4-7-membered heterocyclic ring optionally fused with a 5- to 6-membered carbocyclic or heterocyclic ring; and R3 and R4 are selected from H, C1-8 alkyl, aryl, C5-12 cycloalkyl and aryl-C1-2-alkyl; or R3 and R4 together with the nitrogen atom form a C4-7-membered heterocyclic ring.
Public/Granted literature
- US20100280245A1 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF N-ACYLATED-4-ARYL BETA-AMINO ACID DERIVATIVES Public/Granted day:2010-11-04
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