Patent ID: 7868180

Claim:
A process for the preparation of a sartan derivative of formula (I) wherein can be a single bond or a double bond and wherein if is a double bond, then Y does not exist, R 1 is C 2 -C 7 straight-chain or branched alkyl, C 2 -C 7 straight-chain or branched alkoxy or C 3 -C 9 cycloalkyl, R 2 is hydroxymethyl, formyl, or an optionally substituted carboxyl group, wherein the substituent may be a straight or branched C 1 -C 10 alkyl group, a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group or a C 7 -C 13 aralkyl group, or R 2 is a group of formula X is H, Cl, or X and R 2 , taken together with the double bond of the imidazole ring, form a 6-membered aromatic ring which can be substituted by a carboxyl group which may be further substituted with a straight or branched C 1 -C 10 alkyl group, a C 3 -C 8 cycloalkyl group, a C 6 -C 10 aryl group, a C 7 -C 13 aralkyl group, or a group of the formula and if is a single bond, then R 1 is C 2 -C 7 straight-chain or branched alkyl, R 2 is ═O and X and Y form a C 4 -C 7 cycloalkyl group, or a pharmaceutically acceptable salt thereof, comprising the steps of: reacting 2-cyanophenylboronic acid or a derivative thereof, wherein said 2-cyanophenylboronic acid or derivative is selected from (a) a compound represented by formula (III) wherein the R 3 groups independently stand for H or an unsubstituted or substituted C 1 -C 4 alkyl or a C 6 -C 10 aryl group or wherein two R 3 groups form a 1,2-phenylene group, or an alkali metal salt thereof, (b) a compound represented by formula (IV) wherein n is 0 or 1; and A 1 -A 6 are independently H or an optionally substituted C 1 -C 4 alkyl group, C 3 -C 8 cycloalkyl group or C 6 -C 10 aryl group or (c) a compound represented by formula (V) wherein M is an alkali metal or an NR 4 R 5 R 6 R 7 group wherein R 4 -R 7 are independently H or an unsubstituted or substituted C 1 -C 18 alkyl group in a cross-coupling reaction with a p-halobenzyl-1H-imidazole derivative of formula (VI), wherein , X, Y, R 1 and R 2 are as defined above, and Z is I, Br or Cl, in the presence of a solvent, a transition metal catalyst and an inorganic or organic base to form a substituted biphenyl imidazole compound of formula (II) wherein , X, Y, R 1 and R 2 are as defined above, converting the compound of formula (II) into the corresponding 2-tetrazole derivative to obtain a sartan derivative of formula (I) and, optionally, converting the sartan derivative into one of its pharmaceutically acceptable salts or esters.