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| Study on the synthesis of R-tetrahydropapaverine |
| Jia Hui, Liu Shipu, Chen Feng, Li Xin |
| Shijiazhuang Yike Pharmaceutical Technology Corporation Ltd., Shijiazhuang 050000, China |
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Abstract R - tetrahydropapaverine is an important intermediate of the muscular relaxant cisatracurium besilate. It was synthesized from 3, 4-dimethoxyphenylacetic acid and 3, 4-dimethoxyphenethylamine by three steps of acylation, dehydra-
tion cyclization and reduction, and was broken up with N-acetyl-L-leucine as resolution agent. The results showed that the R-configurationwith a purity of 99.5% was obtained by recrystallization in three steps, and the final yield was about 38%.
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