| 摘要 |
<p>2-Guanidino-4-heterocyclyl-quinazoline derivatives (I) are new. Quinazoline derivatives of formula (I) and their salts, solvates, stereoisomers (including mixtures in all proportions) and derivatives are new; Y = -N=C(NR<5>R<6>)-NR<7>R<8> or -N(R<5>)-C(=NR<6>)-NR<7>R<8>; Het = saturated, unsaturated or aromatic heterocycle (optionally substituted by one or more of R<3> and/or R<4>); R1-R4 = H, A, OA, halo, CF3, CH2CONH2, CH2COOH, CH2COOA, CH2NH2, CH2NA2, CH2NHA, CH2OH, CH2OA, OH, NO2, NH2, NHA, NA2, NHCOA, NHCOPh, SA, SOA, SO2A, SO2Ph, CN, OCF3, COA, COOH, COOA, CONH2, CONHA, CONA2, SO2NH2, SO2NHA, SO2NA2, CHO, phenyl (optionally substituted by one or more of A, OH, OA, halo, CN or CF3), benzyl, cyclohexylmethyl or heterocyclyl (optionally substituted by one or more of A, OH, OA, halo, CN or CF3); A = 1-6C alkyl; R<5>-R<7> = H, benzyl, allyl, another amino-protecting group, A or phenyl (optionally substituted by one or more of A, OH, OA, halo, CN or CF3); and R<5>+R<7>, R<5>+R<6> or R<7>+R<8> = group completing a 5-7 membered ring. Independent claims are also included for: (1) the preparation of (I); and (2) new aniline and chloroquinazoline derivative intermediates of formulae (II) and (IV). All definitions are as above.</p> |
