合成路线:Reaction of 4-acetylpyridine (I) with hot dimethylformamide dimethyl acetal (II) gives the enamino ketone (III),which is then condensed with (3-amino-1H-pyrazol-4-yl)(2-pyridyl)methanone (IV) in boiling acetic acid.Intermediate (IV),(3-amino-1H-pyrazol-4-yl)(2-pyrid-yl)methanone,is obtained by condensation of 3-oxo-3-(2-pyridyl)propionitrile (V) with dimethylformamide dimethyl acetal (II) to provide 2-(dimethylaminomethylene)-3-oxo-3-(2-pyridyl)propionitrile (VI),which is finally coupled with aminoguanidine nitrate (VII) by means of 10N NaOH in refluxing EtOH
合成路线:3-(Acetamido)acetophenone (VII) was converted to enaminone (VIII) upon condensation with dimethylformamide dimethylacetal.The amide N of (VIII) was then alkylated by means of iodomethane and NaH or,alternatively,under phase-transfer conditions to give (IX).Finally,condensation between enaminone (IX) and aminopyrazole (VI) in refluxing AcOH provided the target pyrazolopyrimidine.
参考文献标题:Aryl and heteroaryl 7-(aryl and heteroaryl)-pyrazolo[1,5-a]pyrimidin-3-ylmethanones
文献作者:Dusza,J.P.; Tomcufcik,A.S.; Albright,J.D.(Wyeth)
参考来源:DE 3422844; EP 0129847; JP 1985019788
合成路线:Reaction of 4-acetylpyridine (I) with hot dimethylformamide dimethyl acetal (II) gives the enamino ketone (III),which is then condensed with (3-amino-1H-pyrazol-4-yl)(2-pyridyl)methanone (IV) in boiling acetic acid.Intermediate (IV),(3-amino-1H-pyrazol-4-yl)(2-pyrid-yl)methanone,is obtained by condensation of 3-oxo-3-(2-pyridyl)propionitrile (V) with dimethylformamide dimethyl acetal (II) to provide 2-(dimethylaminomethylene)-3-oxo-3-(2-pyridyl)propionitrile (VI),which is finally coupled with aminoguanidine nitrate (VII) by means of 10N NaOH in refluxing EtOH
参考文献标题:Ocinaplon
文献作者:Castar,J.; Silvestre,J.S.; Chilman-Blair,K.
参考来源:Drugs Fut 2003,28(2),115-120
产品链接: CAS No. 96604-21-6››