Synthetic process of decitabine

地西他滨(Decitabine)的合成工艺

Abstract

The invention relates to a method for preparing Decitabine. The particular proposal for solving the technical problem is as follows: 2-deoxidtion-D-ribose, 10 percent of HCL methanol solution, methoxyacetic acetic anhydride, HMDS, acetic anhydride, tri-silicyl tri-fluorine methane sulfonic acid ester, acetic acid amine, etc. are adopted as raw materials to synthesize the Decitabine; the target product of the Decitabine is obtained through the five steps of reactions, namely, methylation, acylation, trimethyl silication, ammoniation and deacylation with a total yield of above 18.4 percent and a product purity of above 99.7 percent.
本发明涉及地西他滨的制备方法。本发明解决技术问题采用的具体方案是:地西他滨的合成是以2-脱氧-D-核糖、10%HCl甲醇溶液、甲氧基乙酸酐、HMDS、乙酸酐、三甲硅基三氟甲磺酸酯、醋酸胺等为原料,经甲基化、酰化、三甲基硅化、氨化、脱酰化等五步反应得到目标产物地西他滨,总产率大于18.4%,产品纯度大于99.7%。

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Cited By (12)

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    CN-101787046-AJuly 28, 2010上海百灵医药科技有限公司;福建南方制药股份有限公司地西他滨的中间体化合物的制备方法
    CN-101787046-BDecember 26, 2012福建南方制药股份有限公司, 重庆泰濠制药有限公司地西他滨的中间体化合物的制备方法
    CN-101899079-BSeptember 12, 2012鲁南制药集团股份有限公司Preparation, separation and purification method of Decitabine
    CN-101987858-BSeptember 26, 2012上海秀新臣邦医药科技有限公司New method for preparing decitabine beta-configuration intermediate
    CN-103130855-AJune 05, 2013连云港润众制药有限公司一种地西他滨的制备方法
    CN-103130855-BApril 29, 2015连云港润众制药有限公司Preparation method of decitabine
    CN-107011399-AAugust 04, 2017郑州职业技术学院, 河南省生物工程技术研究中心Preparation method of beta-configuration decitabine precursor
    JP-2013506665-AFebruary 28, 2013サイノファーム タイワン リミテッドデシタビンの合成
    US-2010249394-A1September 30, 2010Albemarle CorporationProcesses for producing decitabine
    WO-2010129211-A3February 24, 2011Dr. Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.Préparation de décitabine