Development of a practical synthesis of STA-5312, a novel indolizine oxalylamide microtubule inhibitor

…, Z Xia, S Chen, K Koya, M Ono, L Sun

文献索引：Li, Hao; Xia, Zhiqiang; Chen, Shoujun; Koya, Keizo; Ono, Mitsunori; Sun, Lijun Organic Process Research and Development, 2007 , vol. 11, # 2 p. 246 - 250

全文：HTML全文

被引用次数: 32

摘要

An efficient synthesis of the novel microtubule inhibitor STA-5312 (3-[(4-cyanophenyl) methyl]-N-(3-methyl-5-isothiazolyl)-α-oxo-1-indolizineacetamide) was developed. A novel DMF/Me2SO4 directed regioselective synthesis of the 3-(4-cyanobenzoyl)-indolizine (4) was a critical transformation within the four-step process. Alternatively, a CuCl mediated synthesis of 3-(4-cyanobenzyl) indolizine (5) was also developed. All intermediates were ...