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filingDate 2002-08-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c3aa573ef60e8810f8c415d8f1db640c
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publicationDate 2005-02-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-2005032875-A1
titleOfInvention Process for the preparation of indole derivatives
abstract A process for the preparation of compounds of formula (I) wherein R 1 is unsubstituted or substituted C 1 -C 8 alkyl, R 2 , R 3 , R 4 and R 5 are each independently of the others hydrogen, unsubstituted or substituted C 1 -C 8 alkyl, C 1 -C 8 alkoxy, phenoxy or benzyloxy, or halogen, Y 1 and Y 2 are each independently of the other hydrogen or a protecting group, or Y 1 and Y 2 together form a protecting bridge, and X 1 is hydrogen, an organic radical or a cation, in which process a compound of formula (II) wherein R 1 R 2 , R 3 , R 4 and R 5 are as defined above and Z 1 is a leaving group, is reacted, in the presence of a catalytically effective amount of a palladium catalyst, with a compound of formula (III) wherein R 6 is hydrogen, bromine, chlorine, iodine, —OSO 2 CF 3 , —COCI, —B(OH) 2 or a mono- or di-ester derived from —B(OH) 2 , Y 3 and Y 4 are each a protecting group, or Y 3 and Y 4 together form a protecting bridge, and X 1 is as defined above, to form a compound of formula (IV) and if desired the radicals Y 3 and Y 4 are converted into the radicals Y 1 and Y 2 where Y 1 and Y 2 are hydrogen.
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Total number of triples: 486.