Letters in Organic Chemistry ( IF 0.7 ) Pub Date : 2020-09-30 , DOI: 10.2174/1570178617666200207110526 Pathan Sultan Ismail 1 , Repale Anil Vithal 1 , Girdhar Pal Singh 1
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Celecoxib containing pyrazole derivatives were synthesized by path aldol condensation of substituted ketone with trifluoroethyl acetate subsequently by cyclization of the formed chalcones with 4-methanesulfonylphenylhydrazine. Here, a one-pot synthesis of celecoxib and substituted analogues have been reported which are nonsteroidal anti-inflammatory drugs for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. In order to intermediate work-up, a continuous one-pot synthesis has been developed, performing the entire reaction sequence that results in a shorter time with good yield.
中文翻译：
含吡唑骨架的活性药物成分的原位合成
含有塞来昔布的吡唑衍生物的合成方法是：将取代的酮与三氟乙酸乙酯进行羟醛羟醛缩醛缩合反应，然后将生成的查耳酮与4-甲磺酰基苯肼环化，从而合成出塞来昔布。在此，已经报道了塞来昔布及其取代类似物的一锅法合成，它们是非甾体类抗炎药，具有环氧化酶（COX）抑制，抗炎活性和致溃疡作用。为了进行中间处理，已经开发了一种连续的一锅法合成方法，可以完成整个反应过程，从而缩短反应时间，并获得良好的收率。
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