Patent ID: 7371854
Filing Date: 2008-05-13
Classification: A61P,C07C,C07D

Abstract:
1. A process for preparing a compound of formula I in which R R R R R X is absent or denotes NH, R R R A, A′ each, independently of one another, denote H or alkyl having 1-15 C atoms or cycloalkyl having 3-15 C atoms, each of which is unsubstituted or mono-, di- or trisubstituted by R Ar denotes mono- or bicyclic aromatic ring system having 0, 1, 2, 3 or 4 N, O and/or S atoms which is unsubstituted or mono-, di- or trisubstituted by A and/or R Ph denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by A, Hal denotes F, Cl, Br or I, or a pharmaceutically acceptable salt or solvate, thereof, comprising a) reacting 5-oxotetrahydrofuran-2-carboxylic acid with a compound of the formula II in which R L denotes Cl, Br, I or a free or reactively functionally modified OH group, to give a compound of the formula III in which R b) then reacting a compound of the formula III with a compound of the formula IV in which R L denotes Cl, Br, I or a free or reactively functionally modified OH group, to give a compound of the formula V in which R R c) then reacting a compound of formula III or V with a compound of formula VI in which R R R R R R R A, A′ each, independently of one another, denote H or alkyl having 1-15 C atoms or cycloalkyl having 3-15 atoms, each of which is unsubstituted or mono-, di- or trisubstituted by R Ar denotes mono- or bicyclic aromatic ring system having 0, 1, 2, 3 or 4 N, O and/or S atoms which is unsubstituted or mono-, di- or trisubstituted by A and/or R Ph denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by A, Hal denotes F, Cl, Br or I, to give a compound of formula VII in which R R R R R R R R A, A′ each, independently of one another, denote H or alkyl having 1-15 C atoms or cycloalkyl having 3-15 C atoms, each of which is unsubstituted or mono-, di- or trisubstituted by R Ar denotes mono- or bicyclic aromatic ring system having 0, 1, 2, 3 or 4 N, O and/or S atoms which is unsubstituted or mono-, di- or trisubstituted by A and/or R Ph denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by A, Hal denotes F, Cl, Br or I, d) then converting a compound of formula VII into a compound of formula VIII in which R R R R R R R A, A′ each, independently of one another, denote H or alkyl having 1-15 C atoms or cycloalkyl having 3-15 C atoms, each of which is unsubstituted or mono-, di- or trisubstituted by R Ar denotes mono- or bicyclic aromatic ring system having 0, 1, 2, 3 or 4 N, O and/or S atoms which is unsubstituted or mono-, di- or trisubstituted by A and/or R Ph denotes phenyl which is unsubstituted or mono-, di- or trisubstituted by A, Hal denotes F, Cl, Br or I, e) subsequently, optionally, a compound of the formula VIII is converted into a compound of formula VIIIa in which R L denotes Cl, Br, I or a reactively functionally modified OH group, e) then reacting a compound of the formula VIII or a compound of formula VIIIa e) i) with a compound of formula IX in which R in which R e) ii) with a compound of formula X in which R to give a compound of formula I, subsequently, optionally, converting a radical R in which R L denotes Cl, Br, I or a free or reactively functionally modified OH group, and optionally converting a base or acid of a compound of formula I into one of its pharmaceutically acceptable salts.