TETRAZOLE DERIVATIVES, INTERMEDIATE NITRILES, AND PHARMACEUTICAL COMPOSITIONS

摘要

Compounds of formula IMAGE (I) wherein R1, R2 and R3 are each independently selected from H, OH, C1-C4 alkyl, R4-CO and halogen, where R4 is C1-C4 alkyl; R5 and R6 are each independently selected from H, C1-C4 alkyl and optionally-substituted phenyl; R7 is an alkylene group having from 1 to 4 carbon atoms, optionally containing a substituted or unsubstituted phenyl group; p is 0 or 1; and Z is a 1H-tetrazol-5-yl or a -CN group; and salts thereof, may be prepared by reacting a compound of formula. IMAGE with a compound of formula IMAGE wherein R1-R7 are as defined in claim 1, in an organic solvent at a temperature in the range of 40 DEG -120 DEG C. in the presence of a base, and reacting the resulting compound with an alkali metal cyanide or thiocyanate, and optionally reacting the resulting compound with a source of azide ions to produce pharmacologically active compounds of formula I wherein Z is 1H-tetrazol-5-yl.