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[摘要]:A new and efficient method has been reported for the synthesis of 2-amino-9-[4-acetoxy-3-(acetoxymethyl)butyl-1-yl]purine (famciclovir) starting from guanine. The route involves chlorination of guanine, optimized Mitsunobu reaction, coupling with di-Et malonate, hydrogenation, redn. and esterification, and the overall yield is about 29%. This method does not require any form of chromatog. purifn. to give pure famciclovir, and it is an industrially viable manufg. process for this drug. |
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