申请人:President and Fellows of Harvard College
公开号:US05721362A1
公开(公告)日:1998-02-24
The present invention is directed to a synthetic process for the formation of ecteinascidin compounds and related structures, such as the saframycins. In one particularly preferred embodiment, the present invention provides a synthetic route for the formation of ecteinascidin 743 (1), ##STR1## an exceedingly potent and rare marine-derived antitumor agent which is slated for clinical trials. The process of this invention is enantio- and stereocontrolled, convergent and short. Also disclosed are novel process intermediates, useful not only in the total synthesis of ecteinascidin 743, but also other known ecteinascidin compounds, including derivatives and analogs thereof.
本发明涉及一种合成过程,用于形成ecteinascidin化合物及相关结构,如saframycins。在一个特别优选的实施例中,本发明提供了一种合成途径,用于形成ecteinascidin 743(1),一种极其有效且罕见的海洋来源的抗肿瘤药物,即将进行临床试验。本发明的过程是对映和立体控制的,收敛且短。还披露了新颖的过程中间体,不仅在ecteinascidin 743的全合成中有用,还可用于其他已知的ecteinascidin化合物,包括其衍生物和类似物。