| 摘要 |
A process is provided for preparing pyrazolo[1,5-c]quinazoline derivatives of the structure <IMAGE> wherein X is O or S; R1 is hydrogen, lower alkyl, hydroxymethyl, phenyl-lower alkyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl; R2 is lower alkoxy, phenyl-lower alkoxy, phenoxy, or phenoxy substituted with lower alkyl or lower alkoxy; and R3 and R4 are the same or different and are selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, alkoxy of 1 to 4 carbons, lower alkanoyloxy of 1 to 4 carbons, nitro, benzyloxy, benzyloxy having a single mono-lower alkoxy substituent, halogen, hydroxy, and trifluoromethyl, wherein quinolone compounds of the structure <IMAGE> which are new intermediates, are reacted with a hydrazine compound to form a 5-(2-aminophenyl)pyrazole which is then cyclized to the product. In addition, the above product may be reacted with a halogen acid to form the corresponding hydroxymethyl compound.
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