PYRAZOLO-(1,5a)-PYRIMIDINES, PROCESS FOR PREPARING THE SAME AND THEIR USE.

摘要

Pyrazolo-(1,5a)-pyrimidines have formula (I), in which the indexes and substituents have the following meanings: n equals 0 or 1; Y stands for 0, S, NRa, OCH2*, SCH2*, NRaCH2*, CH2O*, CH2S*, CH2NRa*, CH2CH2, CRa=Rb or CC, the positions with an * indicating the bond to the phenyl ring; R' stands for H3CO-CO-o=CHOCH3, H3CNH-CO-o=CHOCH3, H3CO-CO-o=NOCH3, H3CNH-CO-o=NOCH3, H2N-CO-o=NOCH3, HO-CO-o=NOCH3, H3CO-CO-o=CHCH3, H3CO-CO-o=CHCH2CH3, H3C-CO-o=CHOCH3, H3C-CO-o=NOCH3, H3CCH2-CO-o=NOCH3, in which o indicates a C atom bound to the phenyl ring, N(OCH3)-CO2CH3, N(CH3)-CO2CH3, N(CH2CH3)-CO2CH3, or a group R'.1-o=NOCH3, R'.2-o=NOCH3, R'.3-o=NOCH3 or R'.4-o=NOCH3; m equals 0, 1, 2 or 3; the residues R" may be different when m is greater than 1; R" stands for cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or haloalkylthio; R1, R3 stand for hydrogen, cyano, nitro, hydroxy, amino, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkylthio, alkylthio halide, aryl, arylalkyl, aryloxy, arylalkoxy, arylthio, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkoxy, heteroarylthio or NRcRd, NRcNRdRe, CO-Rc, CO2-Rc, CO-NRcRd, O-CO-Rc, O-CO2-Rc, O-CO-NRcRd, NRc-CO-Rd, NRc-CO2-Rd or NRc-CO-NRdRe; R2 stands for hydrogen, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, aryl, aryloxy, heteroaryl, heteroaryloxy, CO-Rc, CO2-Rc or CRf=NORg; R4 stands for hydrogen, cyano, nitro, nitroso, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkylthio, alkylthio halide, aryl, arylalkyl, aryloxy, arylalkoxy, arylthio, heteroaryl, heteroarylalkyl, heteroaryloxy, heteroarylalkoxy, heteroarylthio or NRcRd, CO-Rc, CO2-Rc or CRf=NORg; Ra, Rb stand for hydrogen, halogen, C1-C4 alkyl or C1-C4 alkyl halide; Rc, Rd and Re stand for hydrogen, alkyl, alkenyl, alkinyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl; Rf stands for hydrogen, cyano, halogen, or optionally substituted alkyl, alkyloxy, alkylthio, alkenyl, alkenyloxy, alkenylthio, alkinyl, alkinyloxy, alkinylthio, cycloalkyl, cycloalkyloxy, cycloalkylthio, heterocyclyl, heterocyclyloxy, heterocyclylthio, aryl, aryloxy, arylthio, heteroaryl, heteroaryloxy or heteroarylthio; Rg stands for hydrogen or optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, heterocyclyl, aryl or heteroaryl. Also disclosed are a process for preparing the same and their use.