Amoxapine, CL-67772, Asendin
阿莫沙平Chemical Name: 2-Chloro-11-(1-piperazinyl)dibenzo[b,f][1,4]oxazepine
CAS No. 14028-44-5
项目整合开发状态: Launched-1980
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:The reaction of O-(p-chlorophenoxy)aniline hydrochloride (I) with ethyl chlorocarbonate (A) in pyridine ether gives ethyl O-(p-chlorophenoxy)phenylcarbanilate (II),which is condensed with N-carbetoxypiperazine (B) by means of Na2O or NaOCH3 in refluxing benzene to afford ethyl 4-[(O-(p-chlorophenoxy)phenyl)carbamoyl]-1-piperazine carboxylate (III).This product is finally decarboxylated and cyclized with P2O5 in refluxing POCl3.
合成路线:The condensation of 11-amino-2-chlorodibenzo[b,f][1,4]oxazepine (IV) with piperazine (A) by means of aluminum chloride at 100 C.
📌 参考资料/链接：
参考文献标题:Amoxapine
文献作者:Playle,A.C.; Castar,J.
参考来源:Drugs Fut 1976,1(11),511
📄 详细内容
合成路线:The reaction of O-(p-chlorophenoxy)aniline hydrochloride (I) with ethyl chlorocarbonate (A) in pyridine ether gives ethyl O-(p-chlorophenoxy)phenylcarbanilate (II),which is condensed with N-carbetoxypiperazine (B) by means of Na2O or NaOCH3 in refluxing benzene to afford ethyl 4-[(O-(p-chlorophenoxy)phenyl)carbamoyl]-1-piperazine carboxylate (III).This product is finally decarboxylated and cyclized with P2O5 in refluxing POCl3.
参考文献标题:Treatment of depression with 2-chloro-11-(pipeazinyl)dibenz[b,f][1,4]oxazepines and acid addition salts thereof
文献作者:Howell,C.F.; et al.
参考来源:BE 0698690; FR 7845M; GB 1192812; GB 1192812; NL 6706970; US 3663696; US 3681357
合成路线:The condensation of 11-amino-2-chlorodibenzo[b,f][1,4]oxazepine (IV) with piperazine (A) by means of aluminum chloride at 100 C.
参考文献标题:Nouveau proc閐?pour la pr閜aration des 11-tert-aminodibenz[b,f][1,4]oxaz閜ines et thiaz閜ines
文献作者:Howell,C.F.; et al.
参考来源:DE 1645954; ES 335760; FR 1508536; US 3444169
产品链接: CAS No. 14028-44-5››