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发明公开
CN110078765A 一种替诺福韦二吡呋酯的制备方法 无效 - 驳回

一种替诺福韦二吡呋酯的制备方法
摘要：
本发明公开了一种替诺福韦二吡呋酯的制备方法，涉及替诺福韦二吡呋酯制备领域。该替诺福韦二吡呋酯的制备方法，具体步骤为：A）(R)-9-（2-羟丙基）腺嘌呤制备；B）(R)-9（2-膦酸甲氧基丙基)腺嘌呤二(乙基)酯制备；C）替诺福韦制备；D）替诺福韦二吡呋酯制备；E）成品检测检验：与现有技术相比，本发明的有益效果是：在保证替诺福韦二吡呋酯药效的同时，缩短了反应步骤，提高了产量，其中各中间产物(R)-9-（2-羟丙基）腺嘌呤、(R)-9（2-膦酸甲氧基丙基)腺嘌呤二(乙基)酯、替诺福韦的转化率分别高达75%、63.2%和74.3%，最终的替诺福韦二吡呋酯的总收率高达62.4%。
摘要（英）：

The invention discloses a method for preparing tenofovir disoproxil and relates to the field of preparation of tenofovir disoproxil. The method for preparing the tenofovir disoproxil specifically comprises the following steps: A) preparing (R)-9-(2-hydroxypropyl) adenine; B) preparing (R)-9-(2-phosphonic acid methoxy-propyl) adenine di(ethyl) ester; C) preparing tenofovir; D) preparing tenofovir disoproxil; and E) carrying out finished product detection and inspection. Compared with the prior art, the method has the beneficial effects that while the medicine effect of the tenofovir disoproxilis ensured, the reaction steps are simplified, the yield is increased, the conversion rates of intermediates (R)-9-(2-hydroxypropyl) adenine, (R)-9-(2-phosphonic acid methoxy-propyl) adenine di(ethyl)ester and tenofovir reach 75%, 63.2% and 74.3% respectively, and the total yield of the tenofovir disoproxil is as high as 62.4% finally.

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