公开(公告)号：US20120065393A1

公开(公告)日：2012-03-15

申请号：US12921820

申请日：2009-02-25

申请人： Byoung-Taek Choi ,  Yun-Beom Ham ,  Seong-Seon Yu ,  Kyung-II Jeong ,  Byung-Sik Kim

发明人： Byoung-Taek Choi ,  Yun-Beom Ham ,  Seong-Seon Yu ,  Kyung-II Jeong ,  Byung-Sik Kim

IPC分类号： C07D498/12

CPC分类号： C07D498/18

摘要： The present invention relates to a process of preparing a highly pure tacrolimus, which comprising a pre-purification process carried out by means of crystallization, and particularly to a process of preparing a highly pure tacrolimus, which comprises a pre-purification process comprising the steps of (a) extracting mycelia cake collected by filtering a tacrolimus-containing oily compound with an organic solvent, (b) concentrating the extract under reduced pressure and (c) crystallizing the concentrate. In addition, a highly pure tacrolimus can be obtained by dissolving the pre-purified crystals in an organic solvent, passing through the solution in an adsorption resin and concentrating the eluate under reduced pressure, followed by crystallization. According to a process of the present invention, Tacrolimus as pure as appropriate for a pharmaceutical purpose can be prepared by a simple process and at a relatively low cost.

摘要翻译： 本发明涉及一种制备高纯度他克莫司的方法，其包括通过结晶进行的预纯化方法，特别涉及一种制备高纯度他克莫司的方法，其包括预纯化方法，其包括步骤 （a）通过用有机溶剂过滤含有他克莫司的油性化合物而收集的菌丝体饼，（b）在减压下浓缩提取物和（c）使浓缩物结晶。 此外，通过将预纯化的晶体溶解在有机溶剂中，通过溶液吸附树脂并减压浓缩洗脱液，然后结晶，可以获得高纯度他克莫司。 根据本发明的方法，可以通过简单的方法并以相对较低的成本制备适合于药物目的的纯粹的他克莫司。