Patent ID: 8785659
Filing Date: 2014-07-22
Classification: A61P,C07D

Abstract:
1. A process for preparing a compound of formula I: wherein R1 is hydrogen, R2 is hydrogen, R3 is hydrogen, R4 is hydrogen, R5 is hydrogen, R6 is -T1-Q1, T1 is a bond, Q1 is Ar1, Aa1, Hh1, or Ah1, Ar1 is phenyl, or R61- and/or R62-substituted phenyl, R61 is 1-4C-alkyl, or -T2-N(R611)R612, either T2 is a bond, and R611 is 1-4C-alkyl, 1-4C-alkoxy-2-4C-alkyl, or phenyl-1-4C-alkyl, R612 1-4C-alkyl, or 1-4C-alkoxy-2-4C-alkyl, or R611 and R612 together and with inclusion of the nitrogen atom, to which they are bonded, form a heterocyclic ring Het1, Het1 is morpholino, thiomorpholino, S-oxo-thiomorpholino, S,S-dioxo-thiomorpholino, piperidino, or pyrrolidino, or T2 is 1-4C-alkylene, or 2-4C-alkylene interrupted by oxygen, and R611 is 1-4C-alkyl, 1-4C-alkoxy-2-4C-alkyl, or phenyl-1-4C-alkyl, R612 is 1-4C-alkyl, or 1-4C-alkoxy-2-4C-alkyl, or R611 and R612 together and with inclusion of the nitrogen atom, to which they are bonded, form a heterocyclic ring Het1, Het1 is morpholino, thiomorpholino, S-oxo-thiomorpholino, S,S-dioxo-thiomorpholino, piperidino, pyrrolidino, imidazole, pyrrolo or pyrazolo, R62 is 1-4C-alkyl, 1-4C-alkoxy, halogen, cyano, 1-4C-alkoxy-1-4C-alkyl, 1-4C-alkylcarbonylamino, or 1-4C-alkylsulphonylamino, Aa1 is a bisaryl radical made up of two aryl groups, which are independently selected from the group consisting of phenyl and naphthyl, and which are linked together via a single bond, Hh1 is a bisheteroaryl radical made up of two heteroaryl groups, which are independently selected from the group consisting of monocyclic 5- or 6-membered heteroaryl radicals comprising one or two heteroatoms, each of which is selected from the group consisting of nitrogen, oxygen and sulfur, and which are linked together via a single bond, Ah1 is a heteroaryl-aryl radical or an aryl-heteroaryl radical made up of a heteroaryl group selected from the group consisting of monocyclic 5- or 6-membered heteroaryl radicals comprising one or two heteroatoms, each of which is selected from the group consisting of nitrogen, oxygen and sulfur, and an aryl group selected from the group consisting of phenyl and naphthyl, wherein said heteroaryl and aryl groups are linked together via a single bond, wherein Aa1, Hh1 and Ah1 may be optionally substituted by R63 and/or R64, R63 is 1-4C-alkyl, phenyl-1-4C-alkyl, 1-4C-alkoxy, trifluoromethyl, cyano, halogen, completely or predominantly fluorine-substituted 1-4C-alkoxy, 1-4C-alkoxy-1-4C-alkyl, 1-4C-alkylsulphonylamino, tolylsulphonylamino, phenylsulphonylamino, 1-4C-alkylcarbonylamino, carbamoyl, mono- or di-1-4C-alkylaminocarbonyl, mono- or di-1-4C-alkylaminosulphonyl, or -T3-N(R631)R632, T3 is a bond, 1-4C-alkylene, or 2-4C-alkylene interrupted by oxygen, R631 is 1-4C-alkyl, 1-4C-alkoxy-2-4C-alkyl, or phenyl-1-4C-alkyl, R632 1-4C-alkyl, or 1-4C-alkoxy-2-4C-alkyl, or R631 and R632 together and with inclusion of the nitrogen atom, to which they are bonded, form a heterocyclic ring Het2, Het2 is morpholino, thiomorpholino, S-oxo-thiomorpholino, S,S-dioxo-thiomorpholino, piperidino, pyrrolidino, imidazole, pyrrolo or pyrazolo, and R64 is 1-4C-alkyl, 1-4C-alkoxy or halogen, comprising reacting an acrylic acid chloride compound of formula II′: wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined for the compound of formula I, with aqueous hydroxylamine, and optionally converting the resulting compound into an acid addition salt thereof.