PROCESS FOR PREPARING 5-AMINOMETHYL-2-THIOPHENECARBONITRILE HCL

摘要

PURPOSE: Provided is a process for effectively preparing 5-aminomethyl-2-thiophenecarbonitrile HCl which is a useful intermediate of oral thrombin inhibitor. CONSTITUTION: The process for effectively preparing 5-aminomethyl-2-thiophenecarbonitrile HCl of the formula(6) comprises the steps of: brominating a compound of the formula(3) to obtain a compound of the formula(4); azidating the compound of the formula(4) to manufacture a compound of the formula(5); and performing Staudinger reaction of iminophosphorane then hydrolysis.