Patent ID: 7521421

Claim:
A cyclosporin A derivative having the structure of Formula (II): wherein the configuration of the MeBmt residue is as shown in FIG. 3 , compound 5 and R is an unsaturated straight or branched aliphatic carbon chain of from 2 to 3 carbons, prepared by a method comprising: (a) protecting the β-alcohol of cyclosporin A, thereby forming an intermediate acetyl cyclosporin A; (b) oxidizing the acetyl cyclosporin A to produce an intermediate acetyl cyclosporin A aldehyde; (c) treating the intermediate acetyl cyclosporin A aldehyde in a Wittig reaction with a phosphorus ylide having the structural formula RCH═PPh 3 wherein R is as defined above to produce an acetyl cyclosporin A derivative having the structure of Formula (I): wherein R is as defined above and the configuration of the MeBmt residue is as shown in FIG. 3 , compound 5; and (d) hydrolyzing the acetyl cyclosporin A derivative having the structure of Formula (I) with a base.