Patent ID: 8846958
Filing Date: 2014-09-30
Classification: A61P,C07C,C07D,C12P,C12Y

Abstract:
1. A process for the synthesis of lubiprostone comprising: a) coupling of cyclopentenone of formula I: with an organocopper compound of formula III: to provide a compound of formula IV: b) reacting the compound of formula IV with hydrogen in the presence of a catalyst to provide a compound of formula V: c) oxidising the compound of formula V to provide a compound of formula VI: d) converting the compound of formula VI to lubiprostone via 1) hydrolysis followed by desilylation or 2) desilylation followed by hydrolysis, wherein R R Li each of n,m and o is 1 or 2 such that either C17 through to C19 is fully saturated or C17 through to C19 contains one single and one double or triple bond, R R