Global Patent Index - EP 2111404 A1

EP 2111404 A1 20091028 - METHOD FOR PRODUCTION OF ARYL-SUBSTITUTED ANNELATED PYRIMIDINES

Title (en)

METHOD FOR PRODUCTION OF ARYL-SUBSTITUTED ANNELATED PYRIMIDINES

Title (de)

VERFAHREN ZUR HERSTELLUNG ARYLSUBSTITUIERTER ANELLIERTER PYRIMIDINE

Title (fr)

PROCÉDÉ DE PRODUCTION DE PYRIMIDINES ANNELÉES, SUBSTITUÉES PAR ARYLE

Publication

EP 2111404 A1 20091028 (DE)

Application

EP 08701400 A 20080110

Priority

  • EP 2008050254 W 20080110
  • EP 07100430 A 20070111
  • EP 08701400 A 20080110

Abstract (en)

[origin: WO2008084082A1] The invention relates to a method for production of aryl-substituted annelated pyrimidines of general formula (I), where L<SUP>1</SUP> to L<SUP>5</SUP>=<SUP/>H, halogen, CN, NO<SUB>2</SUB>, C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl, C<SUB>1</SUB>-C<SUB>4 </SUB>haloalkyl, C<SUB>1</SUB>-C<SUB>4 </SUB>alkoxy, C<SUB>1</SUB>-C<SUB>4 </SUB>haloalkoxy, etc., Y<SUP>1</SUP> to Y<SUP>3</SUP> = C-R<SUP>?</SUP> or N, R<SUP>?</SUP> = H or optionally substituted C<SUB>1</SUB>-C<SUB>4 </SUB>alkyl or two adjacent R<SUP>?</SUP> groups together form a ring, X = OH, Cl or Br, comprising: i) the reaction of a 2-phenylmalonate with a compound (III) or a tautomer thereof, in the presence of a suitable base, with continuous removal of the alcohol of formula R-OH, formed during the reaction, under reduced pressure, to give a compound of formula (I) or a salt thereof, where X = OH and in the case that X in compounds of general formula (I) = chlorine or bromine, ii) the reaction of the compounds of formula (I) obtained in step (i) or the salt thereof with a halogenating agent.

IPC 8 full level

C07D 487/04 (2006.01)

CPC (source: EP US)

C07D 487/04 (2013.01 - EP US)

Citation (search report)

See references of WO 2008084082A1

Designated contracting state (EPC)

AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MT NL NO PL PT RO SE SI SK TR

DOCDB simple family (publication)

WO 2008084082 A1 20080717; CN 101583613 A 20091118; EP 2111404 A1 20091028; JP 2010515706 A 20100513; US 2010087640 A1 20100408

DOCDB simple family (application)

EP 2008050254 W 20080110; CN 200880002186 A 20080110; EP 08701400 A 20080110; JP 2009545180 A 20080110; US 52187708 A 20080110