Patent ID: 7943647

Claim:
A process for the manufacture of a compound of formula (IV b) or a tautomer or a salt thereof, characterized by (i) reacting a compound of formula (IV c) or an ester thereof, with a an azide compound of formula (R 1 )(R 2 )M-N 3 (II b), wherein R 1 and R 2 , independently represent an organic residue selected from the group consisting of an aliphatic residue, an alicyclic residue, a heteroalicyclic residue; an alicyclic-aliphatic residue; a heteroalicyclic-aliphatic residue; a carbocyclic and a heterocyclic aromatic residue; an araliphatic residue or an heteroaraliphatic residue, each residue, independently of another; and M is boron or aluminium; wherein, an aliphatic residue is C 1 -C 20 alkyl, C 3 -C 20 alkenyl or C 3 -C 20 alkynyl, each of which can be interrupted by NH, substituted NH, O, or S; an alicyclic residue is mono-, bi- or polycyclic, selected from the group consisting of C 3 -C 8 cycloalkyl and C 3 -C 7 cycloalkenyl; a heteroalicyclic residue is an alicyclic residue, wherein at least one carbon atom is replaced by a heteroatom selected from the group consisting of NH, substituted NH, O, and S; an alicyclic-aliphatic residue is C 1 -C 20 alkyl, C 3 -C 20 alkenyl or C 3 -C 20 alkynyl that is substituted by C 3 -C 8 cycloalkyl or by C 3 -C 7 cycloalkenyl; a heteroalicyclic-aliphatic residue is C 1 -C 8 -alkyl, C 2 -C 8 -alkenyl or C 2 -C 8 -alkynyl each of which substituted by C 3 -C 8 cycloalkyl or by C 3 -C 8 -cycloalkenyl wherein one carbon atom of C 3 -C 8 cycloalkyl or C 3 -C 8 -cycloalkenyl, respectively, is replaced by NH, substituted NH, O, or S; a carbocyclic aromatic residue selected from the group consisting of moncyclic, bicyclic and polycyclic, or benzoanellated carbocyclic residue; a heterocyclic aromatic residue is 5- or 6-membered and monocyclic radical which has up to four identical or different hetero atoms, selected from the group consisting of nitrogen, oxygen and sulfur atoms, preferably one, two, three or four nitrogen atoms, an oxygen atom or a sulfur atom; an araliphatic residue is C 1 -C 8 -alkyl, C 2 -C 8 -alkenyl or C 2 -C 8 -alkynyl each of which is substituted by phenyl or by naphthyl; an heteroaraliphatic residue is C 1 -C 8 -alkyl, C 2 -C 8 -alkenyl or C 2 -C 8 -alkynyl each of which is substituted by pyrazolyl, imidazolyl, triazolyl, tetrazolyl, furyl, thienyl or pyridyl; and substituted NH is NH which is substituted by C 1 -C 8 -alkyl, phenyl-C 1 -C 8 -alkyl, C 2 -C 8 -alkyl-alkanoyl, phenyl-C 2 -C 5 -alkanoyl, benzoyl, C 1 -C 8 -alkanesulfonyl or benzenesulfonyl; l and M is boron or aluminium; and (ii) isolating the resulting compound of formula (IV b).