Patent ID: 6407258
Filing Date: 2002-06-18
Classification: C07D

Abstract:
A process for the preparation of a compound of the in whichR(1) is hydrogen; alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, which is unsubstituted or is substituted by 1, 2 or 3 identical or different radicals from the group consisting of F, Cl, Br, CF3, methyl, methoxy, NO2 or NR(6)R(7); â€”CnH2n-cycloalkyl having 1, 2, 3, 4, 5, 6 or 7 carbon atoms; where n is equal to 0, 1, 2 or 3; â€”CnH2n-phenyl, which is unsubstituted or is substituted by 1, 2 or 3 identical or different radicals from the group consisting of F, Cl, Br, CF3, NO2, methyl, methoxy, hydroxyl or NR(6)R(7); where n is equal to 0, 1, 2 or 3; or â€”CnH2n-heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, which is unsubstituted or is substituted by 1, 2 or 3 identical or different radicals from the group consisting of F, Cl, Br, CF3, NO2, methyl, methoxy, hydroxyl or NR(6)R(7); where n is equal to 0, 1, 2 or 3; R(2) and R(3) independently of one another are â€”SR(4) or â€”COOR(5); R(4) and R(5) independently of one another are alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, which is unsubstituted or is substituted by 1, 2 or 3 identical or different radicals from the group consisting of F, Cl, Br, CF3, methyl, NO2, methoxy or NR(6)R(7); â€”CnH2n-cycloalkyl having 3, 4, 5, 6 or 7 carbon atoms; where n is equal to 0, 1, 2 or 3; â€”CnH2n-phenyl, which is unsubstituted or is substituted by 1, 2 or 3 identical or different radicals from the group consisting of F, Cl, Br, CF3, CN, NO2, methyl, methoxy, hydroxyl or NR(6)R(7); where n is equal to 0, 1, 2 or 3; or â€”CnH2n-heteroaryl having 1, 2, 3, 4, 5, 6, 7, 8 or 9 carbon atoms, which is unsubstituted or is substituted by 1, 2 or 3 identical or different radicals from the group consisting of F, Cl, Br, CF3, NO2, methyl, methoxy, hydroxyl or NR(6)R(7); where n is equal to 0, 1, 2 or 3; and R(6) and R(7) independently of one another are alkyl having 1, 2, 3 or 4 carbon atoms; or a salt thereof, which comprises cyclizing a compound of the formula II in which R(1), R(2) and R(3) have the meaning defined above, in the presence of an alkylphosphonic anhydride to give a compound of the formula (I), and, optionally, treating the compound of formula (I) with an acid to obtain a salt of the compound of formula (I).