A method of preparing 6-heptyne derivatives of capsaicin of general formula 1, wherein R is a substituent selected from the group comprising C 1 -C 18 straight chain and branched alkyl, C 1 -C 18 straight chain and branched alkenyl, C 1 -C 18 straight chain and branched alkynyl, trifluoromethyl, C 3 -C 12 cycloalkyl, phenoxy, phenylthio, fluoro, chloro, bromo, iodo, phenyl, and substituted phenyl; wherein said substituted phenyl ring is substituted in any one or more positions with 1-5 identical or different substituents selected from the group comprising fluoro, chloro, bromo, iodo, cyano, nitro, trifluoromethyl, C 1 -C 6 straight chain and branched alkoxy, C 1 -C 6 sulfoxy, -S-C 1 -C 6 alkyl, C 1 -C 6 straight chain and branched alkyl, C 2 -C 6 straight chain and branched alkenyl, C 2 -C 6 straight chain and branched alkynyl, C 1 -C 6 fluoroalkyl, chloroalkyl, bromoalkyl, iodoalkyl, COO-C 1 -C 6 alkyl, CONH(C 1 -C 6 alkyl), and CON(C 1 -C 6 alkyl) 2; and R' represents 0-5 identical or different substituents, in any one or more positions, selected from the group comprising fluoro, chloro, bromo, iodo, hydroxy, cyano, amino, nitro, trifluoromethyl, C 1 -C 6 straight chain and branched alkoxy, C 1 -C 6 sulfoxy, -S-C 1 -C 6 alkyl, C 1 -C 6 straight chain and branched alkyl, C 2 -C 6 straight chain and branched alkenyl, C 2 -C 6 straight chain and branched alkynyl, C 1 -C 6 fluoroalkyl, chloroalkyl, bromoalkyl, iodoalkyl, COOH, CONH 2, -NHCO(C 1 -C 6 alkyl), COO-C 1 -C 6 alkyl, CONH(C 1 -C 6 alkyl), and CON(C 1 -C 6 alkyl) 2; the method comprising the step of - coupling a compound of general formula 3 with a benzylamine of general formula 2 or any suitable salt thereof, wherein R and R' for 2 and 3 are defined as for formula 1, using 1,1'-carbonyldiimidazole. R is a substituent selected from the group comprising C 1 -C 18 straight chain and branched alkyl, C 1 -C 18 straight chain and branched alkenyl, C 1 -C 18 straight chain and branched alkynyl, trifluoromethyl, C 3 -C 12 cycloalkyl, phenoxy, phenylthio, fluoro, chloro, bromo, iodo, phenyl, and substituted phenyl; wherein said substituted phenyl ring is substituted in any one or more positions with 1-5 identical or different substituents selected from the group comprising fluoro, chloro, bromo, iodo, cyano, nitro, trifluoromethyl, C 1 -C 6 straight chain and branched alkoxy, C 1 -C 6 sulfoxy, -S-C 1 -C 6 alkyl, C 1 -C 6 straight chain and branched alkyl, C 2 -C 6 straight chain and branched alkenyl, C 2 -C 6 straight chain and branched alkynyl, C 1 -C 6 fluoroalkyl, chloroalkyl, bromoalkyl, iodoalkyl, COO-C 1 -C 6 alkyl, CONH(C 1 -C 6 alkyl), and CON(C 1 -C 6 alkyl) 2; and R' represents 0-5 identical or different substituents, in any one or more positions, selected from the group comprising fluoro, chloro, bromo, iodo, hydroxy, cyano, amino, nitro, trifluoromethyl, C 1 -C 6 straight chain and branched alkoxy, C 1 -C 6 sulfoxy, -S-C 1 -C 6 alkyl, C 1 -C 6 straight chain and branched alkyl, C 2 -C 6 straight chain and branched alkenyl, C 2 -C 6 straight chain and branched alkynyl, C 1 -C 6 fluoroalkyl, chloroalkyl, bromoalkyl, iodoalkyl, COOH, CONH 2, -NHCO(C 1 -C 6 alkyl), COO-C 1 -C 6 alkyl, CONH(C 1 -C 6 alkyl), and CON(C 1 -C 6 alkyl) 2; - coupling a compound of general formula 3 with a benzylamine of general formula 2 or any suitable salt thereof, wherein R and R' for 2 and 3 are defined as for formula 1, using 1,1'-carbonyldiimidazole.