(S)-(-)-氨磺必利-D-(-)-酒石酸盐的合成

张恺1; 薛娜2; 杜玉民1*; 苏信杰1; 周付刚1

引用本文:	张恺1，薛娜2，杜玉民1*，苏信杰1，周付刚1.(S)-(-)-氨磺必利-D-(-)-酒石酸盐的合成[J].中国现代应用药学,2009,(8):635-637.
	ZHANG Kai1, XUE Na2,DU Yumin1*, SU Xinjie1, ZHOU Fugang1.Synthesis of D-(-)tratrate of (S)-(-)-amisulpride[J].Chin J Mod Appl Pharm(中国现代应用药学),2009,(8):635-637.

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(S)-(-)-氨磺必利-D-(-)-酒石酸盐的合成
张恺1，薛娜2，杜玉民1*，苏信杰1，周付刚1

作者	单位
张恺1，薛娜2，杜玉民1*，苏信杰1，周付刚1

摘要:

目的研究(S)-(-)-氨磺必利-D-(-)-酒石酸盐的制备方法。方法以4-氨基-2-甲氧基-5-巯基苯甲酸为原料，经乙基化、氧化得4-氨基-2-甲氧基-5-乙基磺酰基苯甲酸(4)，另由1-乙基-2-氨甲基吡咯烷经D-(-)-酒石酸拆分得S-(-)-1-乙基-2-氨甲基吡咯烷(6)，4与6缩合制得S-(-)-氨磺必利(7)，再与D-(-)-酒石酸成盐制得目标物S-(-)-氨磺必利-D-(-)-酒石酸盐(1)。总收率达25%(以4-氨基-2-甲氧基-5-巯基苯甲酸计算)。结果所得产物经元素分析，红外光谱、核磁共振谱及质谱确证了结构。结论本方法原料易得，反应条件温和，产品质量易控制。

关键词: (S)-(-)-氨磺必利氨磺必利抗精神病药物合成

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Synthesis of D-(-)tratrate of (S)-(-)-amisulpride

ZHANG Kai1, XUE Na2,DU Yumin1*, SU Xinjie1, ZHOU Fugang1

Abstract:

BJECTVIE To study the synthetic method of D-(-)tratrate of (S)-(-)-amisulpride. METHODS (S)-(-)-amisulpride(7) was synthesized from 4-amino-2-methoxy-5-mercaptobenzoic acid via alkylation and oxidation to give 4-amino-2-methoxy-5-ethylsulphonyl benzoic acid(4) which was subjected to condensation with S-(-)-1-ethyl-2-aminomethyl- pyrrolidine(6). Compound 6 was separated from 1-ethyl-2-aminomethyl-pyrrolidine by D-(-)-tartaric acid. The object product (1) was prepared from 7 and D-(-)-tartaric acid via salification with an overall yield of 25% based on 4-amino-2-methoxy-5- mercaptobenzoic acid. RESULTS Chemical structure of product was confimed by element analysis, IR, 1H-NMR and MS. CONCLUSION The process has the advantages of raw material obtained easily, mild reaction, quality controlled easily and suitable for industrial production.

Key words: (S)-(-)-amisulpride amisulpride antipsychotic synthesis