MANUFACTURE OF 4,5,6,7-TETRAHYDROISOZAXOLO[5,4-C]PYRIDIN-3-OL

摘要

The present invention relates to a process for synthesis of 4,5,6,7- tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.