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AN IMPROVED ONE POT PROCESS FOR MAKING KEY INTERMEDIATE FOR GEMCITABINE HCL

机译:制备吉西他滨盐酸盐关键中间体的改进的一锅法

摘要

An improved one pot process for preparing 2-deoxy-D-erythro-2,2-difluoro-pentafuranose-1-ulose-3,5-dibenzoate of Formula (I) comprising hydrolysis of (erythro:threo) alkyl-3-dioxalan-4-yl-2,2-difluoro-3-hydroxy propionate of Formula (III) where alkyl group is having C1-C4 number of carbon atoms using a mild acid and selectively isolating 2-deoxy-D-erythro-2,2-difluoro-pentafuranose-1-ulose-3,5-dibenzoate from the mixture of erythro & threo enantiomers using ethyl acetate, ethylene dichloride and diisopropyl ether as solvents with improved yield and purity.
机译:制备式(I)的2-脱氧-D-赤型-2,2-二氟-呋喃呋喃糖-1-果糖-3,5-二苯甲酸酯的改进的一锅法,该方法包括水解(赤型:苏式)烷基-3-二恶烷。式(III)的-4-基-2,2-二氟-3-羟基丙酸酯,其中烷基使用弱酸并选择性地分离2-脱氧-D-赤-2,2具有碳数为C1-C4的烷基使用乙酸乙酯,二氯乙烷和二异丙醚作为溶剂,从赤型和苏式对映异构体的混合物中制得-二氟戊呋喃糖-1-ulose-3,5-二苯甲酸酯,从而提高了收率和纯度。

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