With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.503614-92-4,1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid,as a common compound, the synthetic route is as follows.,503614-92-4
General procedure: A solution of 5,6-dihydro-3- (4-morpholinyl) -1- [4- (2-oxo-1-piperidinyl) phenyl]2 (1H) -pyridone and ethyl [(4-methoxyphenyl) hydrazino] chloroacetate,In the triethylamine for the acid binding agent under the conditions of condensation, and then by hydrochloric acid deprotection,The resulting intermediates,In the ethylene glycol under high temperature conditions with ammonia reaction in the preparation of an average of apixaban, the purity of 95.4%.In the 50L reactor,Add 2 kg of apixaban crude (purity 95. 4%) and 16L with 10% ammonia in ethylene glycol solution, heated to 90 C dissolved, then add 16L water cooling, stirring at 40 ~ 50 C for 2 hours , Cooling to 0 ~ 10 C. And then filtered to dryness to give 8 kg of a white solid, 90% yield, and an HPLC purity of 99. 97%.
503614-92-4 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid 22240440, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; Zhongmei HuashitongBiotechnology Pharmaceutical Technology (Wuhan) Co.,Ltd; HU, MINGLONG; WU, HAOHAO; CUI, JIAN; QIAN, LINA; (13 pag.)CN106188036; (2016); A;,
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