盐酸舒托必利的合成

SYNTHESIS OF SULTOPRIDE HYDROCHLORIDE

以2-甲氧基-5-乙磺酰基苯甲酸为原料,合成了抗精神病药盐酸舒托必利。首先将2-甲氧基-5-乙磺酰基苯甲酸用甲醇酯化,制得2-甲氧基-5-乙磺酰基苯甲酸甲酯,产物与N-乙基-2-氨甲基四氢吡咯烷进行缩合反应得舒托必利,直接用浓盐酸成盐得盐酸舒托必利。合成路线工艺简便,条件温和,总收率57.5％。

Sultopride Hydrochloride which is an important antipsychotic drug , was Synthesized from 2-methoxy-5-ethylsulfonyl benzoic acid . The procedure involved three steps. Firstly, 2-methoxy-5-ethylsulfonyl benzoic acid was esterified with methyl alcohol to produce 2-methoxy-5-ethylsulfonyl benzoic acid methylester; then, condensation with N-ethyl-2-aminomethyl pyrrolidine, acidifying with hydrochloric acid(37%). The conditions of all reactions were mild and the processes were convenient; the total yield was above 57. 5%.