CAS: 389128-28-3; (2R,5S)-5-(3,4-Dihydro-2,4-Dioxo-1(2H)-Pyrimidinyl)-1,3-Oxathiolane-2-Carboxylic Acid (1R,2S,5R)-5-Methyl-2-(1-Methylethyl)Cyclohexyl Ester

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(1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (2R,5R)-5-(methylcarbonyloxy)-1,3-oxathiolane-2-carboxylate 4-(2,4,6-triisopropylbenzenesulfonyl)uracil-1-yl]-1',3'-oxathiolane-2'(R)-carboxylic acid (1R,2S,5R)-menthyl ester5'(S)-[O4-(2,4,6-triisopropylbenzenesulfonyl)uracil-1-yl]-1',3'-oxathiolane-2'(R)-carboxylic acid (1R,2S,5R)-menthyl ester 4-[1-(4-azidobutyl)]cytosin-1-yl}-1',3'-oxathiolane-2'(R)-carboxylic acid (1R,2S,5R)-menthyl ester5'(S)-{N4-[1-(4-azidobutyl)]cytosin-1-yl}-1',3'-oxathiolane-2'(R)-carboxylic acid (1R,2S,5R)-menthyl ester 4-[1-(4-azidobutyl)]cytosin-1-yl}-2'(R)-dibenzyl-oxyphosphoryloxymethyl-1',3'-oxathiolane5'(S)-{N4-[1-(4-azidobutyl)]cytosin-1-yl}-2'(R)-dibenzyl-oxyphosphoryloxymethyl-1',3'-oxathiolane

📜(2R,5R)-5-羟基-1,3-氧硫杂环-2-羧酸 (1R,2S,5R)-5-甲基-2-异丙基环己酯置于4-二甲氨基吡啶,硫酸氢铵,六甲基二硅氮烷体系中,用 四氢呋喃,氯仿 用作溶剂,化学反应 3.0H,反应生成拉米夫定杂质27
参考文献:一种拉米夫定的工业化制备方法
标题:一种拉米夫定的工业化制备方法
摘要:本发明公开了一种拉米夫定的工业化制备方法,以(2R,5R)‑5‑羟基‑[1,3]‑氧硫杂环戊烷‑2‑羧酸(2S‑异丙基‑5R‑5‑甲基‑1R‑环己基)酯和酰化试剂为原料进行酰化反应,所得产物再与2,4‑二(三甲硅氧基)嘧啶进行糖基化反应,所得产物再与1,2,4‑三氮唑反应得中间体,中间体加入氨水进行氨化反应得酯化合物,最后进行还原反应得拉米夫定产品.该方法原料简单易得,硅试剂用量少,成本低;无乙醚,二氯亚砜等危险试剂的使用,三废污染少;嘧啶保护基在反应完成后可自动脱除,不需要额外的工艺步骤;整个工艺操作简单,收率高,无过柱纯化工艺,适合工业化生产.