Knowledge Center

Patent / 2006

Process for preparation of fluticasone analogs via esterification of a carbothioic acid

Hovione Inter Ltd.

Authors:
  • Luis Sobral
  • William Heggie
Source:
WO 2006043015
A process for prepg. esters, such as I (R = CO(CH2)n, COCHMe2, n = 1, 2), was disclosed and comprised esterification of the C-17 hydroxyl group of 6?,9?-difluoro-11?,17?-dihydroxy-16?-methyl-3-oxoandrosta-1,4-diene-17?-carbothioic acid I (R = H) with a slight excess of a corresponding acyl chloride, RCOCl, inert solvent the presence of a tertiary amine.