合成路线:The condensation of p-anisidine (IV) with 3-chloropropionyl chloride (V) by means of TEA in hot toluene,hot 2-butanone or DMF gives the corresponding amide (VI),which is then cyclized by means of AlCl3 in N,N-dimethylacetamide at 150-60 C and treated with NaBH4 in water to yield the desired 6-hydroxy-1,2,3,4-tetrahydroquinolin-2-one intermediate (III).
参考文献标题:Processes for preparing 6-hydroxy-3,4-dihydroquinolinone,cilostazol and N-(4-methoxyphenyl)-3-chloropropionamide
文献作者:Mendelovici,M.; Nidam,T.; Pilarsky,G.(Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA,Inc.)
参考来源:WO 0170697
合成路线:By reaction of N-[(4-chlorobutyl)carbonyl]cyclohexylamine (I) first with PCl5 and then with NH3 in benzene to give 1-cyclohexyl-5-(4-chlorobutyl)tetrazole (II),which is treated with 6-hydroxy-3,4-dihydrocarbostyril (III) and 1,5-diazabicyclo[5.4.0]undecene-5 (DBU) in ethanol.Alternatively,the condensation can be performed by means of either NaOH,KOH or KOH / K2CO3 in a great variety of solvents.
参考文献标题:Processes for preparing cilostazol
文献作者:Finkelstein,N.; Mendelovichi,M.; Pilarksi,G.(Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA,Inc.)
参考来源:WO 0214283
合成路线:By reaction of N-[(4-chlorobutyl)carbonyl]cyclohexylamine (I) first with PCl5 and then with NH3 in benzene to give 1-cyclohexyl-5-(4-chlorobutyl)tetrazole (II),which is treated with 6-hydroxy-3,4-dihydrocarbostyril (III) and 1,5-diazabicyclo[5.4.0]undecene-5 (DBU) in ethanol.Alternatively,the condensation can be performed by means of either NaOH,KOH or KOH / K2CO3 in a great variety of solvents.
参考文献标题:OPC-13,013
文献作者:Blancafort,P.; Serradell,M.N.; Hillier,K.; Castar,J.
参考来源:Drugs Fut 1982,7(4),264
产品链接: CAS No. 73963-72-1››