从Boc-保护氨基的天冬氨酸苄酯出发,通过5步反应简捷地合成了犬尿氨酸羟化酶的选择性抑制剂L-3-(邻甲氧基苯甲酰基)丙氨酸(o-MBA).其中关键反应为锂试剂对Weinreb酰胺的亲核取代反应.
A concise five-step synthesis of L-3-(o-methoxybenzoyl)alanine, a selective kynurenine hy- droxylase inhibitor is described starting from commercially available 4-benzyl L-N-(tert-butoxycarbonyl) aspartate. Aryl lithium addition to the corresponding Weinreb amide successfully served as the key step.