| 摘要 |
6 9 4-PHENYL-PYRIMIDINE-2-CARBONITRILE DERIVATIVES ABSTRACT. THE INVENTION RELATES TO 4-PHENYI-PYRIMIDINE-2-CARBONITRILE DERIVATIVES HAVING THE GENERAL FORMULA I CIN N'5@K N R2 5 FORMULA I WHEREIN R REPRESENTS 1-3 OPTIONAL SUBSTITUENTS INDEPENDENTLY SELECTED FROM (C,.,)- ALKYL (OPTIONALLY SUBSTITUTED WITH ONE OR MORE HALOGENS), (C,-6)ALKYLOXY (OPTIONALLY SUBSTITUTED WITH ONE OR MORE HALOGENS), CYANO, HALOGEN, HYDROXY, NITRO, (C3.6)CYCLO- ALKYL, CO(C,-6)ALKYL. S(C' 6)ALKYL, SO(C1.6)ALKYL, S02(CL.6)ALKYL, S02NH(CL.8)ALKYL, 10 SO2NH2, NHCO(CL-8)ALKYL AND C02H, OR 2 SUBSTITUENTS R ON ADJACENT POSITIONS REPRESENT TOGETHER OCH20, OCH2CH20 OR CH2CH20. R, IS H OR (CL-6)ALKYLL R2 IS (C2- 6)ALKYL, OPTIONALLY SUBSTITUTED WITH OH, (C,-4)ALKYLOXY, (C6-,O)ARYLOXY, (C6-1O)ARYL(C,- @)ALKYLOXY, ONE OR MORE HALOGENS, NR3R4. C02H OR CONRRR7; R3 AND R4 ARE INDEPENDENTLY H, (CI-8)ALKYL [OPTIONALLY SUBSTITUTED WITH ONE OR MORE HALOGENS, (CL- 15 4)ALKYLOXY OR (C6 LO)ARYLOXY], (C3-8)CYCLOALKYL [OPTIONALLY SUBSTITUTED WITH ONE OR MORE HALOGENSL, (CI 4)ALKYL SUBSTITUTED WITH A 4-8 MEMBERED SATURATED HETEROCYCLIC RING COMPRISING A HETEROATOM SELECTED FROM 0, S AND NR5, A 4-8 MEMBERED SATURATED HETEROCYCLIC RING COMPRISING A HETEROATOM SELECTED FROM 0, S AND NR5, (C6-10)ARYL, (C2-9)HETEROARYL [OPTIONALLY SUBSTITUTED WITH 1-3 SUBSTITUENTS SELECTED FROM HALOGEN, 20 CF3, (CL-4)ALKYL AND (CL-4)AIKYLOXYL, (CE-IO)ARYL(C,@)ALKYL OR (C2Q)HETEROARYL(C1-4)ALKYI. OR R3 AND R4 TOGETHER WITH THE NITROGEN TO WHICH THEY ARE BOUND FORM A 4-8 MEMBERED SATURATED HETEROCYCLIC RING, OPTIONALLY SUBSTITUTED WITH ONE OR MORE HALOGENS OR WITH CONR81R9, AND OPTIONALLY FURTHER COMPRISING I OR MORE HETEROATOMS SELECTED FROM 0, S AND NR5, OR R3 IS H OR (C,,)ALKYL; AND R4 IS (CL-4)ALKYL SUBSTITUTED 2 5 WITH CONR8R9, COOR10, NR8.R9, NRBCOR9, OR NRBCONR9R10; R5 IS H, (CI-4)ALKYL [OPTIONALLY SUBSTITUTED WITH (C3-8)CYCLOALKYL, (C6,LO)ARYL OR (C2 5)HETEROARYL), A- 8)CYCLOALKYL, (C6-,O)ARYL OR (C2-5)HETEROARYL; R6 AND R7 ARE INDEPENDENTLY H, (CL-4)ALKYL OR A 4-8 MEMBERED SATURATED HETEROCYCLIC RING COMPRISING A HETEROATOM SELECTED FROM 0, S AND NR5I OR R6 AND R7 TOGETHER WITH THE NITROGEN TO WHICH THEY ARE BOUND 30 FORM A 4-8 MEMBERED SATURATED HETEROCYCLIC RING, OPTIONALLY SUBSTITUTED WITH ONE OR
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