摘要
以3-氯-1,2-苯并异噻唑和无水哌嗪为原料合成1-(1,2-苯并异噻唑-3-基)哌嗪(2),以6-氯-1,3-二氢-吲哚酮和氯乙酰氯为原料经Friedel-crafts酰化制备5-(2-氯乙酰基)-6-氯-1,3-二氢-吲哚酮(3),3经硼氢化钠和三氟乙酸还原制得5-(2-氯乙基)-6-氯-1,3-二氢-吲哚酮(4),2和4在碘化钠/碳酸钠的水溶液中缩合得到齐拉西酮(1),总收率50.5%(以3-氯-1,2-苯并异噻唑计,n/n)。齐拉西酮的结构经IR和1H NMR确证。
1,2-Benzoisothiazole-3-piperazine（2） was synthesized from 3-chloro-1,2-benzoisothiazole and piperazine.5-（2-Chloroacetyl）-6-chloro-indole ketone（3） was synthesized from 6-chloro-indole ketone and chloroacetyl chloride by Friedel-crafts acylation.Reduction of 3 by sodium borohydride gave 5-（2-chloroethyl）-6-chloro-indole ketone（4）.Combination of 2 and 4 in aqueous solution of NaI / NaCO3 produced ziprasidone（1） in overall yield of 50.5%.The structures were confirmed by IR and 1H NMR.
出处
《精细化工中间体》
CAS
2010年第5期37-39,42,共4页
Fine Chemical Intermediates
