关于13 - 脱氧巴卡亭III的合成研究。

Synthetic studies with 13-deoxybaccatin III.

作者信息

Ahn Yu Mi, Vander Velde David G, Georg Gunda I

机构信息

Department of Medicinal Chemistry and the Drug Discovery Program, Higuchi Biosciences Center, The University of Kansas, Lawrence, Kansas 66045-7582, USA.

出版信息

J Org Chem. 2002 Oct 4;67(20):7140-3. doi: 10.1021/jo011183q.

DOI:10.1021/jo011183q

PMID:12354012

Abstract

An efficient synthesis of 13-epi-7-O-(triethylsilyl)baccatin III from 13-deoxybaccatin III is described. Oxidation of 13-deoxy-7-O-(triethylsilyl)baccatin III with tert-butyl peroxide, followed by reduction with SmI(2), produced 13-epi-7-O-(triethylsilyl)baccatin III in good overall yield. The preparation of 13-oxo-7-O-(triethylsilyl)baccatin III from 13-epi-7-O-(triethylsilyl)baccatin III using tetrapropylammonium perruthenate and N-methylmorpholine N-oxide is also reported.

摘要

描述了一种从13-脱氧巴卡亭III高效合成13-表-7-O-(三乙基甲硅烷基)巴卡亭III的方法。用叔丁基过氧化物氧化13-脱氧-7-O-(三乙基甲硅烷基)巴卡亭III，然后用SmI(2)还原，以良好的总收率得到13-表-7-O-(三乙基甲硅烷基)巴卡亭III。还报道了使用高钌酸四丙铵和N-甲基吗啉N-氧化物从13-表-7-O-(三乙基甲硅烷基)巴卡亭III制备13-氧代-7-O-(三乙基甲硅烷基)巴卡亭III的方法。