申请人:Eisai R&D Management Co., Ltd.
公开号:EP2168961A1
公开(公告)日:2010-03-31
The present invention provides a method for producing a 12-membered ring macrolide compound expected as a prophylactic or therapeutic agent for solid tumors and the like, and a production intermediate thereof. In detail, by acetalizing hydroxyl groups at 6- and 7-positions of a 12-membered ring macrolide compound being a raw material with dialkyl tin (IV) oxide and, after that, reacting the product with a carbamoyl halide derivative, the 7-position urethane derivative of the 12-membered ring macrolide compound being the target is effectively produced, without protecting hydroxyl groups at other positions.
本发明提供了一种生产预期作为固体肿瘤等疾病的预防或治疗剂的12元环大环内酯化合物的方法,以及其生产中间体。具体而言,通过将作为原料的12元环大环内酯化合物的6-和7-位置的羟基与二烷基锡(IV)氧化物缩醛化,然后将产物与氨基甲酰卤衍生物反应,有效地生产了目标为12元环大环内酯化合物的7-位置脲酯衍生物,而无需保护其他位置的羟基。