(Z)-2-(2-三苯甲基氨基噻唑-4-基)-2-[1,5-二(二苯甲氧基)-4-吡啶酮-2-基甲氧基亚胺]乙酸的合成工艺改进
Chinese Journal of Synthetic Chemistry(2016)
Abstract
以5-羟基-2-羟甲基-4-吡喃酮为原料,经羟基保护、迈克尔加成、亲核取代、Mitsunobu反应、肼解及缩合等反应合成了BAL30072关键中间体——(Z)-2-(2-三苯甲基氨基噻唑-4-基)-2-(1,5-二(二苯甲氧基)-4-吡啶酮-2-基甲氧基亚胺)乙酸,总收率23%,其结构经1H NMR和MS确证.该合成工艺已放大到公斤级规模.
MoreKey words
kojic acid,BAL30072,gram-negative bacteria,intermediate,synthesis,process improvement
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