| 摘要 |
6-Unsubstituted 2-amino-4-(bicyclic group-substituted amino)-1,3,5-triazine derivatives (I) and their are new. 1,3,5-Triazine derivatives of formula (I) and their salts are new. R1, R2 = H or NR'R'' (provided that carbon-containing groups R1 and R2 (including substituents) each contain 1-20C); R', R'' = H, alkyl, alkenyl, alkynyl, cycloalkyl, 5-6C cycloalkenyl, Q, OQ, Het, O-Het, S-Het, NH-Het or the acyl residue of a 1-20C organic acid; or NR1R2 = optionally substituted (os), saturated or unsaturated, non-aromatic heterocyclyl, containing 3-9C and 1-4 heteroatoms (i.e. the N of NR1R2 plus 0-3 other N, O or S); Q' = os 1-10C acyclic or cyclic hydrocarbyl; Het = os heterocyclyl, containing 3-9C and 1-3 N, O or S heteroatoms; R3 = H or NH2; NHT, NT2, alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl or heterocyclyl (all os and containing 1-12C including substituents); or an acyl residue of formula -B'-A' (containing 1-12C including substituents); T = 1-4C alkyl; A' = H or Q; B = CO, COO, CONR''', S(O)p or S(O)pO; p = 0-2; R''' = H, alkyl, phenyl, benzyl, cycloalkyl or alkanoyl; R4 = -Z1-R6; R5 = halo, CN, NCO, NO2 or -Z2-R7; or two adjacent groups R5 = group forming a 4-6 membered fused, ring, containing 0-3 O, S and/or N heteroatoms and os by one or more of halo, T and =O; R6 - R9 = H (provided that R7 is not H if Z2 = direct bond), os 1-20C acyclic hydrocarbyl, os cyclic hydrocarbyl or os heterocyclyl; X1 - X4 = C (bonded to H or R5) or N or two adjacent groups X1 - X4 together = O, S or NR3, the ring containing X1 - X4 being a 5- or 6-membered carbocyclic or heterocyclic aromatic ring; each Y1 group = O, CO, C(=NR3), S(O)p, NR3, N(O) or CR8R9 Y2 = as for Y1 or a direct bond, provided that two adjacent groups Y1/Y1 or Y1/Y2 are not both heteroatom groups, the ring containing (Y1)m and Y2 being a 4-8 membered carbocyclic or heterocyclic non-aromatic ring; R8, R9 = as R6, R7 or CR8R9 (in Y1 or Y2) or two groups R8 or R9 (from two groups Y1 or Y2) together = group forming an os 3-8C carbocycle or an os heterocycle; Z1, Z2 = direct bond, O, S(O)p, S()pO, OS(O)p, CO, OCO, COO, NR''', ONR''', NR'''O, NR'''CO or CONR''';and m, n = 0-4. Unless specified otherwise alkyl moieties have 1-6C, alkenyl or alkynyl moieties 1-6C and cycloalkyl moieties 3-6C. Independent claims are included for: (1) the preparation of (I); and (2) new biguanide, amine, isocyanate and triazine compound intermediates of formulae (III), (V), (VII) and (VIII) respectively. R15 = cleavable residue or leaving group. |
