PROCESSES AND INTERMEDIATES FOR PREPARING 5,7-DIHYDRO-3-[2-{1-BENZYLPIPERIDIN-4-YL}ETHYL]-6H-PYRROLO-[4,5-F]-1,2-BENZISOXAZOL-6-ONE

摘要

This invention relates to a process for preparing the compound having formul a (I) which comprises i) heating the compound of formula (VII) wherein R3 is R 4 or benzyl and R4 is R5C(=O), R5OC(=O) or R5SO2 wherein R5 is (C1-C6)alkyl or (C6-C10)aryl(C1-C6)alkyl; at an elevated temperature in the presence of a ba se with the proviso that when R3 in the resultant product is R4 said product is ii) further treated with an aqueous mineral acid at an elevated temperature followed by iii) treatment of the product of ii) with a) a benzylating agent in the presence of a base or b) benzaldehyde in the presence of a reducing agent and an acid.