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    • 5. 发明公开
    • PYRAZOLO- 1,5a]-PYRIMIDINE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG
    • 吡唑并1,5-α]嘧啶,制造方法相同,并且它们的用途
    • EP0824533A1
    • 1998-02-25
    • EP96913532.0
    • 1996-04-26
    • BASF AKTIENGESELLSCHAFT
    • BENOIT, RemyGROTE, ThomasBAYER, HerbertMÜLLER, BerndOBERDORF, KlausSAUTER, HubertAMMERMANN, EberhardLORENZ, GiselaSTRATHMANN, Siegfried
    • A01N43C07D487
    • C07D487/04A01N43/90
    • 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 C C, the positions with an * indicating the bond to the phenyl ring; R' stands for H¿3?CO-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; R?1, 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 NR?cRd, NRcNRdRe, CO-Rc, CO¿2-R?c, CO-NRcRd¿, O-CO-Rc, O-CO¿2-R?c, O-CO-NR?cRd, NRc-CO-Rd, NRc-CO¿2-R?d or NRc-CO-NRdRe; R2¿ stands for hydrogen, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, aryl, aryloxy, heteroaryl, heteroaryloxy, CO-Rc, CO2-R?c 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 NR?cRd, CO-Rc, CO¿2-R?c or CRf=NORg; Ra, Rb¿ stand for hydrogen, halogen, C¿1?-C4 alkyl or C1-C4 alkyl halide; R?c, 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.
    • 6. 发明授权
    • PYRAZOLO- 1,5a]-PYRIMIDINE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG
    • 吡唑并1,5-α]嘧啶,制造方法相同,并且它们的用途
    • EP0824533B1
    • 2001-11-14
    • EP96913532.6
    • 1996-04-26
    • BASF AKTIENGESELLSCHAFT
    • BENOIT, RemyGROTE, ThomasBAYER, HerbertMÜLLER, BerndOBERDORF, KlausSAUTER, HubertAMMERMANN, EberhardLORENZ, GiselaSTRATHMANN, Siegfried
    • C07D487/04A01N43/54
    • C07D487/04A01N43/90
    • 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 C C, the positions with an * indicating the bond to the phenyl ring; R' stands for H¿3?CO-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; R?1, 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 NR?cRd, NRcNRdRe, CO-Rc, CO¿2-R?c, CO-NRcRd¿, O-CO-Rc, O-CO¿2-R?c, O-CO-NR?cRd, NRc-CO-Rd, NRc-CO¿2-R?d or NRc-CO-NRdRe; R2¿ stands for hydrogen, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, aryl, aryloxy, heteroaryl, heteroaryloxy, CO-Rc, CO2-R?c 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 NR?cRd, CO-Rc, CO¿2-R?c or CRf=NORg; Ra, Rb¿ stand for hydrogen, halogen, C¿1?-C4 alkyl or C1-C4 alkyl halide; R?c, 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.