Pazinaclone, A-77000, DN-2327
帕秦克隆Chemical Name: (?-2-(7-Chloro-1,8-naphthyridin-2-yl)-3-[2-(1,4-dioxa-8-azaspiro[4.5]decan-8-yl)-2-oxoethyl]isoindolin-1-one; (?-8-[[2-(7-Chloro-1,8-naphthyridin-2-yl)-2,3-dihydro-3-oxo-1H-isoindol-1-yl]acetyl]-1,4-dioxa-8-azaspiro[4.5]decane
CAS No. 103255-66-9
项目整合开发状态: Phase III
项目研究机构: Takeda (Originator), TAP (Originator)
合成路线:The reaction of 2-(7-chloro-1,8-naphthyrin-2-yl)-3-hydroxyisoindolin-1-one (I) with tert-butoxycarbonylmethylenetriphenylphosphorane (II) in refluxing toluene gives 2-(7-chloro-1,8-naphthyridin-2-yl)-3-oxoisoindolin-1-acetic acid tert-butyl ester (III),which is hydrolyzed with trifluoroacetic acid to the corresponding free acid (IV).Finally,this compound is condensed with 1,4-dioxa-8-azaspiro[4.5]decane (V) by means of diethyl phosphorocyanidate and triethylamine in DMF.
📌 参考资料/链接：
参考文献标题:Isoindolinone derivs.,production and use thereof
文献作者:Goto,G.; Saji,Y.(Takeda Chemical Industries,Ltd.)
参考来源:EP 0174858; JP 1986069773; JP 1990262578; JP 1992364180; US 4778801
📄 详细内容
合成路线:The reaction of 2-(7-chloro-1,8-naphthyrin-2-yl)-3-hydroxyisoindolin-1-one (I) with tert-butoxycarbonylmethylenetriphenylphosphorane (II) in refluxing toluene gives 2-(7-chloro-1,8-naphthyridin-2-yl)-3-oxoisoindolin-1-acetic acid tert-butyl ester (III),which is hydrolyzed with trifluoroacetic acid to the corresponding free acid (IV).Finally,this compound is condensed with 1,4-dioxa-8-azaspiro[4.5]decane (V) by means of diethyl phosphorocyanidate and triethylamine in DMF.
参考文献标题:DN-2327
文献作者:Graul,A.; Prous,J.; Castar,J.
参考来源:Drugs Fut 1993,18(5),414
合成路线:The reaction of 2-(7-chloro-1,8-naphthyrin-2-yl)-3-hydroxyisoindolin-1-one (I) with tert-butoxycarbonylmethylenetriphenylphosphorane (II) in refluxing toluene gives 2-(7-chloro-1,8-naphthyridin-2-yl)-3-oxoisoindolin-1-acetic acid tert-butyl ester (III),which is hydrolyzed with trifluoroacetic acid to the corresponding free acid (IV).Finally,this compound is condensed with 1,4-dioxa-8-azaspiro[4.5]decane (V) by means of diethyl phosphorocyanidate and triethylamine in DMF.
参考文献标题:Benzodiazepine receptor: Demonstration in the central nervous system
文献作者:Okada,T.; Mohler,M.
参考来源:Science 1977,198849-51
产品链接: CAS No. 103255-66-9››