IMPROVED PROCESS FOR THE PREPARATION OF GABAPENTIN ENACARBIL

摘要

Present invention relates to the preparation of highly pure Gabapentin Enacarbil by formation of Gabapentin Enacarbil amine salt US 6,818,787 B2 discloses a process for the preparation of Gabapentin Enacarbil by condensation of 1.-{[(4-nitroph??noxy)carbonyl]oxy}ethyl 2-methylpropanoate with Gabapentin. US 7,232,924 B2 discloses a process for the preparation of Gabapentin Enacarbil starting from Gabapentin and its conversion to allyl/benzyl protected Gabapentin followed by removal of allyl/benzyl protection to furnish Gabapentin Enacarbil. US 8,299,291 B2 discloses a process for the preparation of Gabapentin Enacarbil by condensation of 1-({[4-(methanesulfonyl)phenoxy]carbonyl}oxy)ethyl 2-medrylpropanoate with Gabapentin. US 7,227,028 B2 discloses a process for the preparation of Gabapentin Enacarbil hy condensation of l-({[(2,5-dioxopyrrolidin-1-yl)oxy]carbonyl}oxy)ethyl 2-methylpropanoate with Gabapentin. IN 2013CH00416 discloses a process for the preparation of Gabapentin Enacarbil by condensation of 1-{[(4-nitrophenoxy)carbonyl]oxy}ethyl 2-methylpropanoate with Gabapentin and further purification of Gabapentin Enacarbil by conversion to various amine addition salts such as tert-butylamine, benzylamino and dibenzylamine salts.