| 3-(S)-(-)-(1-氨甲酰基-1,1-二苯甲基)吡咯烷酒石酸盐的制备 |
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| 引用本文： | 廖云凤,翁志洁,李建其. 3-(S)-(-)-(1-氨甲酰基-1,1-二苯甲基)吡咯烷酒石酸盐的制备[J]. 中国医药工业杂志, 2011, 42(5) |
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| 作者姓名： | 廖云凤 翁志洁 李建其 |
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| 作者单位： | 中国医药工业研究总院上海医药工业研究院,上海,200437 |
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| 基金项目： | 国家"重大新药创制"科技重大专项 |
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| 摘 要： | 以L-苹果酸(2)为原料,经与苄胺缩合、还原、氢解脱苄、磺酰化、烷基化、脱保护基、水解后成盐制得氢溴酸达非那新关键中间体3-(S)-(-)-(1-氨甲酰基-1,1-二苯甲基)吡咯烷酒石酸盐,总收率约22%(以2计).
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| 关 键 词： | 3-(S)-(-)-(1-氨甲酰基-1,1-二苯甲基)吡咯烷酒石酸盐 达非那新 中间体 合成 |
Synthesis of 3-(S)-(-)-(1-Carbamoyl-1, 1-diphenylmethyl)pyrrolidine Tartrate |
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| LIAO Yunfeng,WENG Zhijie,LI Jianqi. Synthesis of 3-(S)-(-)-(1-Carbamoyl-1, 1-diphenylmethyl)pyrrolidine Tartrate[J]. , 2011, 42(5) |
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| Authors: | LIAO Yunfeng WENG Zhijie LI Jianqi |
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| Affiliation: | LIAO Yunfeng,WENG Zhijie,LI Jianqi(Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 200437) |
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| Abstract: | 3-(S)-(-)-(1-Carbamoyl-1,1-diphenylmethyl)pyrrolidine tartrate,the intermediate of darifenacin hydrobromide,was synthesized from L-(-)-malic acid by condensation with benzylamine,and then reduction,debenzylation,sulfonylation,alkylation,deprotection,hydrolysis and salt formation with an overall yield of about 22%. |
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| Keywords: | 3-(S)-(-)-(1-carbamoyl-1 1-diphenylmethyl)pyrrolidine tartrate darifenacin intermediate synthesis |
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