| 摘要 |
1-Phenyl-2-aminomethylnaphthalene derivatives (I), are new. 1-Phenyl-2-aminomethylnaphthalene derivatives of formula (I) and their salts and solvates are new. R1, R2 = 1-18C alkyl, 1-18C cycloalkyl, aryl, heteroaryl or benzyl (all optionally substituted at least mono substituted), alkenyl, optionally heteroatom- or aryl-substituted acyl (e.g. formyl, acetyl, trichloroacetyl, fumaryl, maleoyl, succinyl or benzoyl), OR, N(R)2 or SR, or NR1R2 = N-containing ring (optionally at least mono substituted); R = aryl, heteroaryl or benzyl (optionally at least mono substituted) or optionally heteroatom- or aryl-substituted acyl (e.g. formyl, acetyl, trichloroacetyl, fumaryl, maleoyl, succinyl or benzoyl), and R3, R4 = at least one of 1-18C alkyl, 1-18C cycloalkyl, aryl, heteroaryl or benzyl (all optionally at least mono substituted), H, alkenyl, optionally heteroatom- or aryl-substituted acyl (e.g. formyl, acetyl, trichloroacetyl, fumaryl, maleoyl, succinyl or benzoyl) , alkoxy (e.g. OMe, OEt, OnPr, iPr, OnBu, OiBu, OsecBu or OtBu), cycloalkoxy, alkylthio (e.g. SMe or SEt), sulfonyl (e.g. SO3H, SO2Me, SO2CF3, SO2phenylMe or SO2phenylCH2Br), nitrogen-containing group (e.g. amino (optionally substituted by 1 or 2 alkyl or aryl), CN, isocyano or nitro), fluoro, chloro, bromo, iodo or a hetero substituent. Provided that the following compounds are excluded, where: (1) R3 = H; R4 = 2-benzyloxy-4,6-dimethyl or 2-hydroxy-4,6-dimethyl and NR1R2 = amino, di(n-butyl)amino or mono- or di-methylamino; (2) R4 = H; R3 = 4-ethoxy and NR1R2 = N+Me2(CH2CH2OPh) or N+Et2(CH2CH2OPh); (3) R4 = H; R3 = 4-methoxy or 4-ethoxy and NR1R2 = N+Me2(CH2CH2OPh); (4) R4 = H; R3 = 4-hydroxy or 4-methoxy and NR1R2 = 4-butylpiperazino; (5) R4 = H; R3 = 4-methoxy or 4-(2-dimethylbutylammonio-ethoxy) and NR1R2 = 1,4,4-tributylpiperazinium dication; (6) R4 = H; R3 = 4-methoxy or 4-ethoxy and NR1R2 = 4-ethoxycarbonylpiperazino; (7) R4 = H; R3 = 3-methyl and NR1R2 = trimethylammonium or dimethylamino; (8) R4 = H; R3 = 4-methoxy or 4-phenoxy and NR1R2 = 4-phenylpiperazino; (9) R4 = H; R3 = 3-morpholinomethyl and NR1R2 = morpholino; (10) R4 = H; R3 = 4-methoxy and NR1R2 = 4-(2-methylphenyl)piperazino, and (11) R3 = 4-deutero-3-trideuteromethyl and NR1R2 = CD2-NMe2. An Independent claim is also included for the preparation of (I).
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