Efficient Preparation of a Key Intermediate in the Synthesis of Roxifiban by Enzymatic Dynamic Kinetic Resolution on Large Scale
作者:Jaan A. Pesti、Jinguao Yin、Lin-hua Zhang、Luigi Anzalone、Robert E. Waltermire、Philip Ma、Edward Gorko、Pat N. Confalone、Joseph Fortunak、Charlotte Silverman、John Blackwell、J. C. Chung、Michael D. Hrytsak、Mary Cooke、Lakisha Powell、Charles Ray
DOI:10.1021/op0300239
日期:2004.1.1
Additional information is presented for the transformation of a kinetic resolution into a dynamic kinetic resolution of the isobutyl ester 5b to form the acid 2 in high yield and ee via the intermediacy of a thioester 6c, (Pesti, J. A.; Yin, J.; Zhang, L.-H; Anzalone, L. J. Am. Chem. Soc. 2001, 123, 11075−11076.). The development of optimized reaction conditions for the preparation of 6c, its dynamic
提供了关于将异丁酯 5b 的动力学拆分转化为动态动力学拆分的其他信息,以通过硫酯 6c 的中间体以高产率和 ee 形成酸 2,(Pesti,JA;Yin,J.;Zhang , L.-H; Anzalone, LJ Am. Chem. Soc. 2001, 123, 11075−11076.)。描述了制备 6c 的优化反应条件的开发,其动态动力学分辨率为 2,以及将两种反应扩大到中试装置。