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萘丁美酮化学名为4-(6-甲氧基-2-萘基-2-丁酮(1)是非留体消炎镇痛解热药。对肠胃道刺激性较轻,易于耐受。从2-溴-6-甲氧基萘开始,与3-丁烯-2-醇(2)或3-丁烯-2-酮(甲基乙烯酮,3)在钯催化下进行偶合分别以1步法或2步法得到成品1。与2反应时选用催化剂为(ph_3P)_3PdCl~2或ph_3P加Pd(OAc)_2,另加NaHCO_3在1-甲基-2-吡咯烷酮(NMP)中140℃反应5小时,1的收率分别为65和60%。不饱和醇4可能为中间体,经异构化而生成1。与3反应时催化剂为(ph_3P)_2PdCl_2,在NMP中加压130℃反应3小时,得收率90%
Naphtybutynone chemical name is 4- (6-methoxy-2-naphthyl-2-butanone (1) is a non-systemic anti-inflammatory analgesic antipyretics. Irritant to the gastrointestinal tract, easy to tolerate. Coupling with 3-buten-2-ol (2) or 3-buten-2-one (methylketene, 3) under palladium catalysis starting with 2-bromo- 1-step method or 2-step method to get the finished product 1. The reaction with 2 catalyst (ph_3P) _3PdCl_2 or ph_3P plus Pd (OAc) _2, plus NaHCO_3 in 1-methyl-2-pyrrolidone (NMP) 140 ℃ for 5 hours, the yield of 1 were 65 and 60%, respectively.Unolvable alcohol 4 may be an intermediate and isomerized to form 1. The catalyst was (ph_3P) _2PdCl_2 when reacted with 3 and was pressurized 130 ℃ for 3 hours, the yield was 90%