A facile one-pot synthesis of the very useful building blocks N-Boc-S-alkylatedcysteines
作者:Sante Cundari、Renato Dalpozzo、Antonio De Nino、Antonio Procopio、Giovanni Sindona、Kostantinos Athanassopulos
DOI:10.1016/s0040-4020(99)00528-1
日期:1999.8
A convenient one-pot method for the synthesis of N-Boc protected S-alkylcysteines, useful intermediates for the solution-phase synthesis of glutathione-conjugates and modified peptides is presented, together with the reactivity of epoxides, halohydrins and alpha-halo carbonyl derivatives towards the sulfur nucleophile of the substrate. The reactions with alpha-halo esters lead to thiomorpholinocarboxylic acids which are interesting potential inhibitors of transport systems. (C) 1999 Elsevier Science Ltd. All rights reserved.