| 摘要 |
Quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I), their enantiomers, diastereomers and salts are new. A = bond, 1-6C alkylene, 2-6C alkenylene, 2-6C alkynylene, T, A1-T, T-A1, A1-T-A1, or A1-T-A'1-T'; T, T' = carbonyl, carbonyloxy, thio, sulfirylsulfonyl, oxy, amino, 1-6C aminoalkyl, aminoaryl, carbonylamino, carbonylamino-1-6C alkyl, carbonylaminoaryl, oxycarbonyl, aminocarbonyl, 1-6C aminoalkylcarbonyl, aminoarylcarbonyl, sulfonylamino, sulfonylamino-1-6C alkyl, sulfonylaminoaryl, aminosulfonyl, amino-1-6C alkylsulfonyl or aminoarylsulfonyl; A1, A'1 = 1-6C alkylene, 2-6C alkenylene or 2-6C alkynylene; B = 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, arylaminoaryl or aryl-1-6C alkylaryl (all optionally substituted by 1-3 Z); D = 1-6C alkylene (where 1 C atom may be substituted by B); X = O or S; Z, R1 = halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl or 1-6C alkoxycarbonylamino; R2 = H, or 1-6C alkyl, aryl, 3-10C cycloalkyl, Het1, Het2, aryl-1-6C alkyl or Het2-1-6C alkyl-3-10C cycloalkyl-1-6C alkyl or Het1-1-6C alkyl (all optionally substituted by halo, 1-6C alkyl, 1-6C alkoxy, OH, SH, CN, NO2, NH2, 1-6C alkylamino, di-1-6C alkylamino, 1-4C perhaloalkyl, carboxy, 1-6C alkoxycarbonyl, aminocarbonyl, 1-6C alkylaminocarbonyl, di-1-6C alkylaminocarbonyl, carbamoyl, 1-6C alkoxycarbonylamino, or aryl-1-6C alkyl or arylamino (both optionally substituted by 1-3 Z)); aryl = phenyl, naphthyl or biphenyl; Het1 = 5-7 membered saturated or partially unsaturated mono- or polycyclic heterocycloalkyl containing 1-3 N, O or S atoms; Het2 = 5-11 membered mono- or bicyclic aromatic ring containing 1-3 N, O or S; m = 0-4; and n = 0-3; provided that when the 2 N atoms of the imidazol ring are substituted, the imidazole moiety becomes a cationic imidazolium moiety. An Independent claim is also included for the preparation of (I). |
