(+)-AG-041R的不对称合成

Asymmetric Synthesis of(+)-AG-041R

手性氮杂季碳3-氨基吲哚酮结构单元具有多种生物活性和广泛的药用价值。本文以靛红为起始原料,经氨基保护、雷福尔马茨基反应、脱保护、酰化和环化等反应,最终以8步29.1%的总收率得到(+)-AG-041R。反应路线中的每个中间体化合物及目标产物的结构都经过质子核磁共振谱(1H NMR)鉴定。

Chiral a zaquaternary carbon 3-amino-indolone structural units have many biological activities and widely medicinal value. In this paper, a synthetic route of(+)-AG-041 R was designed with isatin as the starting material within 8 steps, which includes amino protection, reformatsky reaction, deprotection, acylation and cyclization with a total yield of 29.1%. The structures of all intermediates and the target molecular in this synthetic route were confirmed by Proton Nuclear Magnetic Resonance(1 H NMR).