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消炎痛(Ⅰ)为常用的解热镇痛药,但有头昏、恶心、胃痛、腹泻等副反应。1980年Boltze等合成了消炎痛醋酸(Acemetacin),化学名:〔1-(4一氯苯甲酰)-5-甲氧基-2-甲基-3-吲哚基乙酰氧基〕醋酸。本品对大白鼠的抗炎作用比消炎痛强一倍,而对猫的口服半数致死量及对狗的静注半数致死量,均为消炎痛的两倍左右。用于临床对人体的抗炎、镇痛、解热作用比消炎痛强或相似;对肠胃道及中枢神经系统的副反应发生率明显低于消炎痛,患者易于耐受。本品的合成路线如下:
Indomethacin (Ⅰ) is commonly used antipyretic analgesics, but there are dizziness, nausea, stomach pain, diarrhea and other side effects. In 1980, Boltze et al. Synthesized Acemetacin with the chemical name: [1- (4-chlorobenzoyl) -5-methoxy-2-methyl-3-indolylacetoxy] acetic acid. The anti-inflammatory effect of this product is twice as strong as anti-inflammatory in rats, and the oral half of the lethal dose of cats and intravenous injection of the median lethal dose, both indomethacin twice. For clinical use on the human body anti-inflammatory, analgesic, antipyretic effect stronger or similar than the anti-inflammatory; gastrointestinal and central nervous system side effects were significantly lower than the incidence of indomethacin, patients with easy tolerance. This product is synthesized as follows: