血管紧张素转化酶抑制剂-盐酸喹那普利的合成新工艺研究.pdfVIP

盘管紧张素转化酶麴豢《刘一鼓酸睦那善零j懿合成囊丁麓硪究 was of UnderthesecondRions。the51．1％．ThebettercondRions were鹅 yield hydrogenization 4,0 follows：theof10％Pd—C tool ester,reaction dosage g船。10 phenylmethyl temperature25℃， reaction 1 2 time72h．Underthese ofNEPAwas MPa,reaction condRions，the pressure yield 80．8％． Thebetterconditionsoftheactivationof were鑫sfollows：” NEPA磅tri砖osgene these time30h．Under ofthe conditions，the 州EPA)：n(tfiphosgene)=1．0：1．3，refluxing yield 92．7％．The conditionsofthecondensationofthe was better N-carboxyanhydride and were8s N-carboxyanhydridephenytmelhyl follows： time6h，reaction 20 t,2，3，4-tetrahydro一3一isoquinolinecarboxylate产l。0：l。t，reactiontemperature of ofthe these was89．晰．Thebetterconditions ℃．Under conditions，the yield hydrogenization esterwereasfollows：theof10％Pd-C3．2 mol above gjo．01 ester,reaction dosage phenylmethyl 72h．Underthese was69．5％．TheactivationofNEPA time conditions,the throughN-earboxy yield hasseveral as low andso