【药物名称】
化学结构式(Chemical Structure):
参考文献No.625972
标题:The effect of 1,3-diaryl-[1H]-pyrazole-4-acetamides on glucose utilization in ob/ob mice
作者:Bebernitz, G.R.; Argentieri, G.; Battle, B.; Brennan, C.; Balkan, B.; Burkey, B.F.; Eckhardt, M.; Gao, J.; Kapa, P.; Strohschein, R.J.; Schuster, H.F.; Wilson, M.W.; Xu, D.D.
来源:J Med Chem 2001,44(16),2601
合成路线图解说明:

Condensation between 4-acetylbiphenyl (I) and 3-(trifluoromethyl)phenyl hydrazine (II) provided the corresponding hydrazone (III). Subsequent Vilsmeier-Haack reaction of (III) with POCl3 and DMF afforded the pyrazole aldehyde (IV). This was subjected to a Knoevenagel condensation with malonic acid to give the pyrazolylacrylic acid (V). Treatment of (V) with sulfur and ammonium hydroxide under Willgerodt-Kindler conditions led to the pyrazolylacetamide derivative (VI), which was further hydrolyzed to carboxylic acid (VII) using H2SO4 in aqueous HOAc. After conversion of (VII) to the corresponding acid chloride (VIII), condensation with dimethylamine in CH2Cl2 gave the title amide.

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