CAS: 122111-01-7; ((2R,3R)-3-(Benzoyloxy)-4,4-Difluoro-5-Oxotetrahydrofuran-2-yl)Methyl Benzoate

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3-(2,2-二甲基-1,3-二氧戊环-4-基)-2,2-二氟-3-羟基丙酸乙酯置于吡啶,盐酸,4-二甲氨基吡啶体系中,用 水 用作溶剂,化学反应 8.0H,反应生成2-脱氧-2,2-二氟戊呋喃糖-1-酮 3,5-二安息香酸盐
参考文献:一种吉西他滨中间体的高选择性的合成方法
标题:一种吉西他滨中间体的高选择性的合成方法
摘要:本发明公开了一种吉西他滨中间体的高选择性的合成方法,具体包括如下工艺:具体包括如下工艺:Step1,T1的合成;Step2,T2的合成,将t1中滴加550Kg双氧水,控制反应生成t2;Step3,T3的合成:向反应釜中加三水乙酸钠或者碳酸钠,用冰醋酸调节ph值,滴加10‑15%次氯酸钠水溶液,控制反应生成t3;Step4,T4的合成;Step5,T5的合成;Step6,T6的合成;Step7,T7的合成;Step8,T8的合成;Step9,T8构型转化;本吉西他滨中间体的高选择性的合成方法能够节省生产成本,同时还能够提高吉西他滨中间体的收率.

专利信息

专利号:WO-9721719-A1
优先权日:1995-12-13
标 题 :α, α-DIFLUORO-β-HYDROXY THIOL ESTERS AND THEIR SYNTHESIS
发明人：WEIGEL JOHN A
权利人:LILLY CO ELI; WEIGEL JOHN A
摘要:A process to make α, α-difluoro-β-hydroxy thiol esters of formula (IIIA), comprising reacting a difluoroethanethioate of formula (IVA), with a second reactant selected from the group consisting of aldehydes, ketones, acid halides and esters; in a solvent and in the presence of a strong base; with the proviso that the process is conducted in the absence of a catalyst and in the absence of a silyl containing compound is described and claimed. The α, α-difluoro-β-hydroxy thiol esters can be useful in the syntheses of organic compounds including gemcitabine hydrochloride.