摘要
报道了以2乙氧基苯腈、DL丙氨酸为原料合成出一种名为伐地那非(Vardenafil)的选择性磷酸二酯酶(Ⅴ)抑制剂。对决定反应总收率的关键步骤———两步成环法进行了讨论,首次分离出了该方法的中间体4,对所有反应条件进行了优化。目标产物及各有机中间体的1HNMR均与文献一致。
A selective phosphodiesterase (Ⅴ) inhibitor called Vardenafil was synthesized by using 2-ethoxybenzonitrile and DL-alanine as the raw materials. The two ring-closing reaction which is the decisive procedure of the whole synthesis was discussed and a new intermediate 4 was first separated. All the reaction conditions were optimized and all NMR spectrum data of the target molecule and intermediates are the same as those of reported.
出处
《化学试剂》
CAS
CSCD
北大核心
2006年第5期287-289,共3页
Chemical Reagents