http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2370592-T3

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filingDate 2009-03-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2011-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a7b0d5da09cc3452bfd0cee5b00dff12
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2308838d90be2dd10508d9f80bdfb75f
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publicationDate 2011-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2370592-T3
titleOfInvention NEW PROCEDURE FOR THE PRODUCTION OF SULPHONYL PIRROLES AS HDAC INHIBITORS.
abstract Process for the preparation of a compound of formula I: wherein R 1 is hydrogen, C 1-4 alkyl, halogen or C 1-4 alkoxy, R 2 is hydrogen or C 1-4 alkyl, R 3 is hydrogen or C 1-4 alkyl, R4 is hydrogen, C1-4 alkyl, halogen or C1-4 alkoxy, R5 is hydrogen, C1-4 alkyl, halogen or C1-4 alkoxy, R6 is T1-Q1, in which T1 is a bond, Q1 is Ar1, Aa1, Hh1 or Ah1, in which Ar1 is phenyl, or phenyl substituted with R62 and / or R61, in which R61 is C1-4 alkyl, or -T2-N (R611) R612, in which or T2 is a bond, and R611 is C1-4 alkyl, C1-4 alkoxy-C2-4 alkyl or phenyl C1-4 R612 is C1-4 alkyl or C1-4 alkoxy-C2-4 alkyl, or R611 and R612 together and including the Nitrogen atom, to which they are attached, form a heterocyclic ring Het1, in which Het1 is morpholino, thiomorpholino, S-oxo-thiomorpholino, S, S-dioxo-thiomorpholino, piperidino or pyrrolidino, or T2 is C1-4 alkylene, or C2-4 alkylene interrupted by oxygen, and R611 is C1-4 alkyl, C1-4 alkoxy C2-4 yl or phenyl-C1-4 alkyl R612 is C1-4 alkyl or C1-4 alkoxy-C2-4 alkyl, or R611 and R612 together and including the nitrogen atom, to which they are attached, form a heterocyclic ring Het1, in which Het1 is morpholino, thiomorpholino, S-oxo-thiomorpholino, S, S-dioxo-thiomorpholino, piperidino, pyrrolidino, imidazolo, pirrolo or pyrazolo, R62 is C1-4 alkyl, C1-4 alkoxy, halogen, cyano , C1-4 alkoxy-C1-4 alkyl, C1-4 alkylcarbonylamino, or C1-4 alkyl sulfonylamino, Aa1 is a bisaryl radical consisting of two aryl groups, which are independently selected from a group consisting of phenyl and naphthyl, and which are linked to each other by a single bond, Hh1 is a bisheteroaryl radical formed by two heteroaryl groups, which are independently selected from a group consisting of monocyclic heteroaryl radicals of 5 or 6 links comprising one or two heteroatoms, each of which which is selected from the group consisting of n itrogen, oxygen and sulfur, and which are linked together by a single bond, Ah1 is a heteroaryl-aryl radical or an aryl-heteroaryl radical formed by a heteroaryl group selected from a group consisting of monocyclic heteroaryl radicals, of 5 or 6 links 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 a group consisting of phenyl and naphthyl, said heteroaryl and aryl groups being linked between yes by a single bond, in which Aa1, Hh1 and Ah1 can be optionally substituted by R63 and / or R64, in which R63 is C1-4 alkyl, phenyl C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, cyano , halogen, C1-4 alkoxy completely or predominantly substituted with fluorine, C1-4 alkoxy-C1-4 alkyl, C1-4 alkyl sulfonylamino, tolylsulfonylamino, phenylsulfonylamino, C1-4 alkylcarbonylamino, carbamoyl, mono- or di-alkyl C1-4-aminocarb nyl, mono- or di-C1-4 alkyl-aminosulfonyl, or -T3-N (R631) R632, wherein T3 is a bond, C1-4 alkylene, or C2-4 alkylene interrupted by oxygen, and R631 is alkyl C1-4, C1-4 alkoxy-C2-4 alkyl or phenyl-C1-4 alkyl, R632 C1-4 alkyl, or C1-4 alkoxy-C2-4 alkyl, or R631 and R632 together and including the nitrogen atom , to which they are linked, form a heterocyclic Het2 ring, in which Het2 is morpholino, thiomorpholino, S-oxo-thiomorpholino, S, S-dioxo-thiomorpholino, piperidino, pyrrolidino, imidazolo, pirrolo or pyrazolo, and R64 is C1 alkyl -4, C1-4 alkoxy or halogen, which comprises the step of reacting an acrylic acid chloride compound of formula II ': in which R1, R2, R3, R4, R5 and R6 have the meanings defined above, with aqueous hydroxylamine and, optionally, convert the resulting compound into an acid addition salt thereof.
priorityDate 2008-03-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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