沙坦联苯的高效合成

Highly Efficient Synthetic Method for Sartan Biphenyl

沙坦类药物是临床上备受关注的一类新型抗高血压药物。沙坦联苯是沙坦类药物的关键中间体。以邻氯苯氰和对甲基苯硼酸为原料,通过对反应溶剂、反应温度、反应时间、催化剂、碱等关键条件的优化,开发了一个合成沙坦联苯的催化体系。此催化体系以PEG400为反应介质,以Pd(OAc)2为催化剂,以K2CO3、Na2CO3或K3PO4为碱,在60℃下反应24 h,沙坦联苯的产率可达99%。该体系是一个绿色、简单、高效合成沙坦联苯的催化体系,为沙坦联苯的合成提供了一个有效的新方法。

Sartan drug is a new type of antihypertensive drug which has been paid much attention in clinic.Sartan biphenyl is a key intermediate for sartan drugs.To develop a new and efficient synthetic method for sartan biphenyl,the effects of solvent,reaction time,catalyst and base on the reaction of o-chlorobenzonitrile and p-tolylboronic acid was investigated.By optimizing above reaction conditions,a green,simple and highly efficient catalytic system for the synthesis of sartan biphenyl was developed.Using PEG400 as solvents and Pd(OAc)2 as catalysts,sartan biphenyl could be obtained in 99%yield in the presence of K2 CO3,Na2 CO3 or K3 PO4 at 60℃for 24 h.