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