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发明公开
CN106046055A R‑9‑(2‑膦酰甲氧基丙基)‑腺嘌呤一水合物晶体及制备、富马酸替诺福韦二吡呋酯制备 无效 - 驳回 转让

R‑9‑(2‑膦酰甲氧基丙基)‑腺嘌呤一水合物晶体及制备、富马酸替诺福韦二吡呋酯制备
摘要：
本发明提供了一种R‑9‑(2‑膦酰甲氧基丙基)‑腺嘌呤一水合物晶体，本发明晶体纯度高、质量好，能够用于进一步制备高质量的富马酸替诺福韦二吡呋酯。同时，本发明还提供了一种所述R‑9‑(2‑膦酰甲氧基丙基)‑腺嘌呤一水合物晶体的制备方法，本发明方法所用原料易得，且操作简便，晶体产率高、质量好；同时，本发明方法中通过分批加料等操作步骤，也进一步提高了所述晶体的产率。进一步的，本发明还提供了一种富马酸替诺福韦二吡呋酯的制备方法，本发明方法中，以本发明所制得的高纯度R‑9‑(2‑膦酰甲氧基丙基)‑腺嘌呤一水合物晶体为原料，从而可以制得高质量的富马酸替诺福韦二吡呋酯产物，并具有产物产量好，操作方法简便等优点。
摘要（英）：

The invention provides R-9-(2-phosphonomethoxy propyl)-adenine monohydrate crystals. The crystals are high in purity and good in quality and can be used for further preparing high-quality tenofovir disoproxil fumarate. Meanwhile, the invention further provides a preparation method of the R-9-(2-phosphonomethoxy propyl)-adenine monohydrate crystals and a preparation method of the tenofovir disoproxil fumarate. The preparation method of the R-9-(2-phosphonomethoxy propyl)-adenine monohydrate crystals has the advantages that the method is easy in raw material obtaining, simple to operate, high in crystal yield and good in crystal quality, and the yield of the crystals is further increased by operation steps such as batch material adding. The preparation method of the tenofovir disoproxil fumarate has the advantages that the prepared high-purity R-9-(2-phosphonomethoxy propyl)-adenine monohydrate crystals are used as the raw materials to prepare the high-quality tenofovir disoproxil fumarate, and the method is good in product quality, simple to operate and the like.

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