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本发明公开了一种拉米夫定中间体HDMS的合成制备方法,通过发明一套乙醛酸薄荷醇酯CME-I的合成工艺,使得该步合成收率大为提高,产品质量稳定,从而是拉米夫定中间体HMDS成本大大降低。乙醛酸薄荷醇酯CME-I合成过程中,通过亚硫酸氢钠和甲醛的加成反应,使得在反应的过程中,反应条件温和,除了回流进行酯化后,操作基本上处于常温条件。乙醛酸薄荷醇酯CME-I合成过程中,仅酯化和萃取时使用环己烷作溶剂,其余均
The invention discloses a synthetic preparation method of lamivudine intermediate HDMS. Through the invention of a glyoxylic menthyl glycolate CME-I synthesis process, the synthesis yield of the step is greatly improved and the product quality is stable so that HMDS cost of lamivudine intermediate is greatly reduced. Glyoxylate menthyl CME-I synthesis process, through the addition of sodium bisulfite and formaldehyde reaction, making the reaction process, the reaction conditions mild, except for reflux esterification, the operation is basically at room temperature conditions. Glyoxylic acid menthol ester CME-I synthesis process, only the esterification and extraction of cyclohexane as a solvent, the rest were