发明名称 PROCESS AND INTERMEDIATES FOR THE PREPARATION OF N-ACYLATED-4-ARYL BETA-AMINO ACID DERIVATIVES
摘要 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.
申请公布号 EP2381772(B1) 申请公布日期 2016.08.24
申请号 EP20090837169 申请日期 2009.12.30
申请人 CHIRAL QUEST, INC. 发明人 WU, SHULIN;YU, BO;WANG, YEJING;DELICE, ALAIN;ZHU, JINGYANG
分类号 C07B53/00;C07C269/06;C07C271/22;C07D487/04 主分类号 C07B53/00
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