Yu Zhu-ming
2012
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Journal
Chemistry & Bioengineering
Abstract
(R)-1-(6-Amino-9H-purin-9-yl)propan-2-ol was one of the key intermediates of Tenofovir Disoproxil Fumarate.It was synthesized starting from 9H-purin-6-amine and(R)-2-methyloxirane.The effects of(R)-2-methyloxirane amount,reaction temperature,catalyst,9H-purin-6-amine concentration,crystallization solvent and crystallization temperature on yield and purity of the target compound were investigated.And the optimum reaction conditions were obtained as follows:the molar ratio of(R)-2-methyloxirane to 9H-purin-6-amine was 1.75∶1,the reaction temperature was 85 ℃,the catalyst was NaOH,9H-purin-6-amine concentration was 1.38 mol·L-1,the crystallization solvent was PrOH-DMF-MeOH(4∶2∶1),the crystallization temperature was-20 ℃,the yield and purity of the target compound reached 69% and 98.6%,respectively.The method was simple in operation and was easy in final treatment of product with high yield,so it was more suitable for industrial production.