| 摘要 |
A process for the racemization of an enantiomerically-enriched compound of formula (3), comprises treatment of enantiomerically-enriched (3) with a base to obtain anion (4), optionally in protonated form, which is then combined with CH2=CH-Y1 to form racemic (3), X(Ar)(Ak)C(CH2)2Y (3) <IMAGE> (4) wherein Ar=aryl or heteroaryl; Ak=C1-20 alkyl; X=CN, CO2R, CONR1R2, and COR; Y and Y1 are independently selected from CN, CO2R, CONR1R2 and R, R1 and R2 are independently selected from H and C1-20 alkyl; optionally as a salt thereof. This racemization process can be used as part of an efficient synthesis of enantiomerically-enriched verapamil or aminoglutethimide. |
