The improvement for synthesis of centchroman

Ji Xioshen

Chinese Pharmaceutical Journal ›› 1998, Vol. 33 ›› Issue (02) : 109-110.

Chinese Pharmaceutical Journal ›› 1998, Vol. 33 ›› Issue (02) : 109-110.
药物化学

The improvement for synthesis of centchroman

  • Ji Xiaoshen
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Abstract

OBJECTIVE: To improve the synthesis and promote the yield for centchroman. METHODS: The reported synthetic route was simplified and redesigned, especially using 2, 2-dimethyl-3-phenyl-7-methoxychromene (2) to react with phenol. RESULTS: The transisomer was got in the step of highly stereo-selective Friedel-Crafts alkylation and final product centchroman was got just by five steps with over all yield of 40%. CONCLUSION: The synthesis for centchroman was simplified and yield was increased with out two steps of hydrogenation in high pressure and configuration transformation which appeared in the reported route.

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centchroman / technical improvement

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Ji Xioshen . The improvement for synthesis of centchroman [J]. Chinese Pharmaceutical Journal, 1998, 33(02): 109-110

References

1 Lyer SS.India launches the new weekly contraceptive pill.Drug News Perspect,1991,4(4):228. 2 Ray S,Grover PK,Anand N.A new synthesis of cis-& trans-3-phenyl-4-[4-(β-pyrrolidinoethoxy)-phenyl]-7-methoxy-chromans.Indian J Chem,1971,9(7):727. 3 Jamas W B.Process for preparation of substituted 3,4-(diphenyl) chromans.US Pat,3,822,287.1974-07-02. 4 季小慎,严久凤,王雪峰.7-甲氧基-3-苯基香豆素的合成中国医药工业杂志,1996,27(3):133.

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