| 摘要 |
1-Benzoyl-3-(heterocyclyl-phenyl)-urea derivatives (I) are new. Benzoylurea derivatives of formula (I) and their salts are new. R1, R2 = H, alkyl (optionally substituted by OH, OT, NH2, NHT or dialkylamino), alkoxy, alkylcarbonyl, alkoxycarbonyl, carboxyalkyl or alkoxycarbonylalkyl; T = 1-4C alkyl; R3, R4 = F, Cl, Br, OH, NO2 or CN; or alkyl, OT, alkenyloxy or alkynyl (all optionally multiply substituted by F, Cl or Br); R5 = H, F, Cl, Br, OH, NO2, CN or COOH; or alkyl, OT, alkylcarbonyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkylsulfonyl, alkenyloxy or alkynyl (all optionally multiply substituted by F, Cl or Br); A = H, F, Cl, Br, OH, NO2, CN, COOH, CONH2, SO2NH2 or NHCOR6; or alkyl, alkylcarbonyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkylsulfonyl, alkenyl, alkynyl, alkoxy, alkylsulfinyl, mono- or dialkylaminocarbonyl, mono- or dialkylaminosulfonyl (all optionally multiply substituted by F, Cl, Br, COOH, alkoxycarbonyl, CONH2, mono- or dialkylaminocarbonyl or alkylcarbonyloxy); R6 = H, alkyl, cycloalkyl, cycloalkyl-(1-4C) alkyl, alkenyl, alkynyl, alkoxycarbonylalkyl, alkylcarbonylalkyl, COOH, carboxyalkyl, carbamoylalkyl, 6-10C aryl, (6-10C) aryl-(1-4C) alkyl, heteroaryl, heteroaryl-(1-4C) alkyl or heteroaryl-carbonyl (where alkyl, cycloalkyl, alkenyl and alkynyl moieites are optionally multiply substituted by F, Cl, Br, OT, COOT or NT2; and aryl or heteroaryl moieties are optionally multiply substituted by F, Cl, Br, NO2, CN, OT, SCOOT, NT2 or alkyl); n, p = 0-3; m = 1-5; Het = 4-7 membered heterocycle containing 1-4 of N, O and/or S as heteroatom(s) (excluding pyrrole), substituted by R7 - R9; and R7 - R9 = H, F, Cl, Br, OH, =O, NH2, COOH or CONH2; or alkyl, alkoxy, alkenyloxy, alkynyloxy, mono- or dialkylamino, alkylcarbonyl, alkoxycarbonyl, mono- or diaklylaminocarbonyl, aryl, aralkyl or alkoxycarbonylalkyl (all optionally multiply substituted by COOH, CONH2, mono- or dialkylaminocarbonyl, alkylcarbonyloxy, F, Cl, alkyl or alkoxy); or two of R7 - R9 may together complete a fused ring. Alkyl moieties have 1-6C, cycloalkyl moieties 3-7C and alkenyl or alkynyl moieties 2-6C unless specified otherwise. An Independent claim is included for the preparation of (I). |
