SELVARAJ NAICKER,RANDALL W YATSCOFF,ROBERT T FOSTER,MARK ABEL,SEETHARAMAN JAYARAMAN,HANS JURGEN MAIR,JEAN MICHEL ADAM,BRUNO LOHRI
申请号：
IN5103/DELNP/2011
公开号：
IN2011DN05103A
申请日:
2011.07.04
申请国别(地区):
IN
年份:
2012
代理人:
摘要：
A method of producing an E-isomer enriched mixture of cyclosporin A analogs modified at the 1-amino acid residue, wherein the stereoselective synthesis of the E-isomer enriched material comprises the steps of (a) reacting an acetyl cyclosporin A aldehyde with a reagent selected from the group consisting of Y-(trialkylsilylallyl) boronate esters and E-y-(trialkylsilylallyl) dialkylboranes to form a ß-trialkylsilyl alcohol (b) treating the ß-trialkylsilyl alcohol with acid to form acetyl-(E)4,3-diene and (c) treating the acetyl-(E)-l,3-diene with base to form the (E)-isomer of ISATX247.
