Clodoxopone, LR-19731

氯氧喷Chemical Name: 4-(4-Chlorophenyl)-5-[2-(4-phenyl-1-piperazinyl)ethyl]-1,3-dioxol-2-one; 4-(p-Chlorophenyl)-5-beta-(N'-phenyl)piperazinoethyl-1,3-dioxol-2-one
CAS No. 71923-34-7, 71923-01-8 (diHCl)
项目整合开发状态: Biological Testing
项目研究机构: Lusofarmaco (Originator)
合成路线:3) By direct cyclization of (I) with phosgene in refluxing CHCl3.
📌 参考资料/链接:
参考文献标题:4-aryl-5-aminoalchil-1,3-dissol-2-oni,loro derivati,processi per la loro preparazione,e composizioni farmaceutche che li contengono
文献作者:Manghisi,E.; Porta,R.; Cascio,G.; Fregnan,G.(Lusofarmaco)
参考来源:BE 0874561

📄 详细内容


合成路线:1) The esterification of 1-(4-chlorobenzoyl)-3-(4-phenyl-1-piperazinyl)propanol (I) with phosgene by means of triethylamine in CHCl3 gives the corresponding chloroformate ester (II),which is then cyclized by heating.

合成路线:2) By direct cyclization of (I) with N,N'- carbonyldiimidazole (III) in refluxing benzene.

合成路线:3) By direct cyclization of (I) with phosgene in refluxing CHCl3.

合成路线:Cyanoacetic acid (I) is condensed with urethane (II) in hot Ac2O to afford N ethoxycarbonyl-cyanoacetamide (III).Subsequent reaction of (III) with triethyl orthoformate yields alpha-cyano-beta-ethoxy-N-ethoxycarbonyl-acrylamide (IV).The ethoxy group of (IV) is then displaced with hydrazine hydrate in EtOH to produce the hydrazino acrylamide (V).Finally,thermal cyclization of (V) gives rise to the title pyrazolopyrimidine (1,2).

参考文献标题:Process for the preparation of biologically active cpds.as well as novel cpds.
文献作者:Shaw,G.; Baildon,S.; Lees,P.Sr.
参考来源:DE 1814082


合成路线:1) The esterification of 1-(4-chlorobenzoyl)-3-(4-phenyl-1-piperazinyl)propanol (I) with phosgene by means of triethylamine in CHCl3 gives the corresponding chloroformate ester (II),which is then cyclized by heating.

合成路线:2) By direct cyclization of (I) with N,N'- carbonyldiimidazole (III) in refluxing benzene.
参考文献标题:N-phenylpiperazine derivatives with hypocholesterolemic activity
文献作者:Gascio,G.; Manghisi,E.; Porta,R.; Fregnan,G.
参考来源:J Med Chem 1985,28(6),815


产品链接: CAS No. 71923-34-7››

产品链接: CAS No.71923-01-8››