| abstract |
The present invention relates to a process for the preparation of phenylethanolamine derivatives; The invention relates in particular to compounds of the formula (I) and salts, solvates or pharmaceutically acceptable derivatives thereof, wherein m is an integer of 2 to 8; a poor number, is 2-5; with the proviso that the value of m + n together is 4-10; R1 is hydrogen, C1-6 alkyl, hydroxy, halo, C1-6 haloalkyl, -XC (O) NR9R10, -XNR8C (O) R9, -XNR8C (O) NR9R10, -XNR8SO2R9, -XSO8SO2N9R10 -XNR9R10, - XN + R8R9R10, -XNR8C (O) OR9, -XCO2R9, -XNR8C (O) NR8C (O) NR9R10, -XSR9, -XSOR9, and -XSO2R9; or R 1 is -X-aryl, -X-heteroaryl, or -X- (aryloxy), each optionally substituted with 1 or 2 identical or different groups of hydroxy, C 1-6 alkoxy, halogen, C 1-6 alkyl, C 1-6 haloalkyl, -NHC (O) (C 1-6 alkyl), -SO 2 (C 1-6 alkyl), -SO 2 (aryl), -SO 2 NH 2, -SO 2 NH (C 1-6 alkyl), -SO 2 NH (C 3-7 cycloalkyl), -CO 2 H, -CO 2 (C 1-6) 6a1ki1), -SO2NH (C3-7cycloalkylC1-6alkyl), -NH2, -NH (C1-6alkyl); or heteroaryl optionally substituted with 1 or 2 or one or more groups of hydroxy, C 1-6 alkoxy, halogen, C 1-6 alkyl, or C 1-6 haloalkyl; X is - (CH 2) p - or C 2-6 alkenylene group p is an integer from 0 to 6 R 8 and R 9 is independently hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, aryl, heteroaryl; heteroaryl (C 1-6 alkyl) - or aryl (C 1-6 alkyl) and R 8 and R 9 are independently optionally substituted by 1 or 2 halogen, C 1-6 alkyl, C 1-6 haloalkyl, -NHC (O) (C 1-6 alkyl), -SO 2 (C 1-6 alkyl), -SO 2 (aryl), -CO 2 H, -CO 2 (C 1-4 alkyl), -NH 2, -NH (C 1-6 alkyl), aryl (C 1-6 alkyl), aryl (C 2-6 alkenyl) -, aryl (C 2-6 alkynyl) -, heteroaryl (C 1-6 alkyl) -, -NHSO 2 aryl, -NH (heteroarylC 1-6 alkyl), -NHSO 2 heteroaryl, -NHSO 2 (C 1-6 alkyl), - NHC (O) aryl, or Of NHC (O) heteroaryl R 10 is hydrogen, C 1-6 alkyl or C 3-7 cycloalkyl; R11 and R12 are independently hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl, heteroaryl, heteroaryl (C1-6alkyl) or aryl (C1-6alkyl), or R11 and R12 together with the nitrogen to which they are attached; A 5, 6, or 7 membered nitrogen ring; and R 11 and R 12 are optionally substituted with one or two groups of halogen, C 1-6 alkyl and C 1-6 haloalkyl; wherein R 1 is -NNR 8 C (O) NR 9 R 10 and R 8 and R 9 together with the -NC (O) N portion of the attached R 1 group may form a 5, 6 or 7 unsaturated or unsaturated ring; wherein R 1 is -XNR 8 C (O) OR 9, and R 8 and R 9 may be taken together with the -NC (O) O portion of the associated R 1 group to form a 5, 6 or 7-membered saturated or unsaturated ring; wherein R 1 is -XC (O) NR 9 R 10 or -XNR 8 C (O) NR 9 R 10 and R 9 and R 10 may be taken together with the nitrogen atom to which they are attached to form a 5, 6, v |