一种新型拉唑类化合物吡美拉唑的合成

Synthesis of a new prazole compound pymeprazole

以2,3-二甲基-4-氯-N-氧代吡啶(1)为起始原料,与3-甲氧基丙醇缩合反应得中间体2,中间体2再与醋酐反应得中间体3,经水解、氯化后得中间体4,中间体4与5缩合反应得硫醚6,最后经氧化得吡美拉唑(7),总收率16%。吡美拉唑结构通过1HNMR、MS方法进行了确认。

A new prazole compound pymeprazole has been designed and synthesized by using 2, 3-dimethyl-4-chloro-N-oxo-pyridine （1） as start matarial, which reacts with 3-methoxy propanol to afford intermediate 2. Then the reaction of intermediate 2 with acetic anhydride provides intermediate 3. The intermediate 4 was obtained by hydrolysis and chlorination, the condensation of the formed inter- mediate 4 with 5 produces sulfide 6. The final oxidation of 6 gives pymeprazole （7）. The overall yield is 16%. The structure of pymeprazole has been characterized by 1HNMR and MS.