申请人:TAISHO PHARMACEUTICAL CO., LTD
公开号:EP1310506A1
公开(公告)日:2003-05-14
There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C-O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.
本发明提供了一种有助于高效合成 6-O-取代酮烷内酯衍生物的制备工艺,该工艺的特 点是将通过选择性裂解 9-位侧环缩醛的 C-O 键而在 6-位引入取代基的步骤与 6、9-环缩醛 5-O-去氨基红曲内酯衍生物,在 9-和 3-位上转化为羰基的步骤,以及 11,12- 环碳化的步骤,从而得到 6-O-取代的酮内酯衍生物。