Patent ID: 7126026
Filing Date: 2006-10-24
Classification: C07C

Abstract:
1. A process for preparing compounds of the formula I wherein: R1 is hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms, alkoxy having 1, 2, 3 or 4 carbon atoms, NR10R11, —O R10 and R11 are, independently of one another, hydrogen, alkyl having 1, 2, 3 or 4 carbon atoms or —CH m is zero, 1 or 2 n, o, p, q, r and s are, independently of one another, zero or 1; R2 is —(SO h is zero, 1 or 2; z is zero or 1; k is zero, 1, 2, 3 or 4; l is zero or 1; or R2 is —(CH t is zero, 1, 2, 3 or 4; u is zero or 1; v is zero, 1, 2 or 3; or R2 is —(CH w is zero, 1, 2, 3 or 4; x is zero or 1; y is zero, 1, 2 or 3; and R3 and R4, independently of one another, are hydrogen or F; and the salts thereof, said process comprising the steps of: a) reducing a 4-nitrophenylsulfur pentafluoride compound to a 4-aminophenylsulfur pentafluoride compound; b) halogenating the 4-aminophenylsulfur pentafluoride compound in the ortho position to the amino group with a halogenating agent; c) replacing the halogen substituent added in step b) with an R2 radical by reacting the 4-aminophenylsulfur pentafluoride compound with a nucleophile or an organometalic compound; d) replacing the amino group added in step a) with a halogen by reacting the 4-aminophenylsulfur pentafluoride compound with a halogenating agent; e) replacing the halogen substituent added in step d) with a nitrile functional group; f) hydrolyzing the nitrile function to a carboxylic acid group; and g) converting the carboxylic acid group to an acylguanidine compound of formula I, wherein R2 is as previously defined.