Ha H J, Park G S, Ahn Y G, Lee G S
Department of Chemistry, Hankuk University of Foreign Studies, Yongin, Kyunggi-Do, Korea.
Bioorg Med Chem Lett. 1998 Jul 7;8(13):1619-22. doi: 10.1016/s0960-894x(98)00271-6.
Practical large scale synthesis of N-benzoyl-(2R,3S)-phenylisoserine methyl ester of the Taxol side chain has been attained from the coupling of chiral imine of N-[(S)-methylbenzyl]benzaldimine with (Z)-alpha-methoxy trimethylsilyl ketene acetal followed by the sequential reactions of lactamization, demethylation, methanolysis and N-benzoylation.
通过N-[(S)-甲基苄基]苯甲醛亚胺的手性亚胺与(Z)-α-甲氧基三甲基硅基乙烯酮缩醛的偶联反应，随后依次进行内酰胺化、脱甲基化、甲醇解和N-苯甲酰化反应，已实现了紫杉醇侧链N-苯甲酰基-(2R,3S)-苯基异丝氨酸甲酯的实际大规模合成。
