申请人:Tapestry Pharmaceuticals, Inc.
公开号:US10238621B2
公开(公告)日:2019-03-26
Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G′ or Formula M′:
with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
本文提供了用于治疗癌症患者癌症的化合物、含有该化合物的组合物和方法。特别是,这些化合物的制造过程包括处理由式 G′或式 M′代表的第一种化合物:
用通式 R8R9C(OCH3)2 的第二种化合物和选自樟脑磺酸 (CSA)、对甲苯磺酸 (PTSA)、盐酸 (HCl) 和乙酸 (AcOH) 的一组酸,其中 R1 和 R2 各自选自 H、烷基、烯烃基、芳香基、O-烷基、O-烯烃基或 O-芳香基;R7 是烷基、烯烃基或芳香族基团;P1 是羟基保护基团;P5 是 H 或位于 7-O 位的易酸保护基团;R8 是 H、烷基、烯烃基或芳香族基团;以及 R9 是:H、烷基、烯烃基或芳香基,或如说明书中所定义。