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| 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 |
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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.
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Received: 14 January 2015
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2016, Vol. 24 
