Process Improvement on the Synthesis of (Z)-2-(2-tritylaminothiazol-4-yl)-2-(1,5-dibenzhydryloxy-4-pyridon-2-ylmethoxyimino)acetic Acid
TAO Yun-liang1, YANG Yu-she2, WANG Hai-dong1,3
1. School of Petrochemical Engineering, Changzhou University, Changzhou 213164, China; 2. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; 3. College of Biological, Chemical Sciences and Engineering, Jiaxing University, Jiaxing 314000, China
Abstract：The key intermediate of BAL30072, (Z)-2-(2-tritylaminothiazol-4-yl)-2-［(1,5-dibenz-hydryloxy）-4-pyridon-2-ylmethoxyimino］acetic acid with overall yield of 23%, was synthesized by protection of phenolic hydroxyl group, Michael addition, nucleophilic substitution, Mitsunobu reaction, hydrazinolysis, condensation reaction and so on, using kojic acid as the starting material. The structure was confirmed by 1H NMR and MS.
陶匀亮， 杨玉社， 汪海东. (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[J]. 合成化学, 2016, 24(1): 75-78.
TAO Yun-liang, YANG Yu-she, WANG Hai-dong. Process Improvement on the Synthesis of (Z)-2-(2-tritylaminothiazol-4-yl)-2-(1,5-dibenzhydryloxy-4-pyridon-2-ylmethoxyimino)acetic Acid. Chinese Journal of Synthetic Chemistry, 2016, 24(1): 75-78.
2016, Vol. 24 
