Indolyl carboxylic anhydrides

Abstract

Abstract Novel anhydrides of the formula <FORM:1069775/C2/1> in which R1 is an aromatic radical of one ring or two fused rings in which any heteroatoms are N, O or S and in which any substituents are halogen, C1- 5 alkyl, C1- 5 alkylthio, C1- 5 alkoxy, trifluoromethyl, phenoxy, (C1- 5 alkyl) -phenoxy, (C1- 5 alkoxy) - phenoxy, halogenophenoxy, mono-, di- or tri-fluoroacetyl, di-(C1- 5 alkyl) sulphamoyl, C1- 6 alkanoyl, di-(C1- 5 alkyl) carboxamido, cyano, carb-C1- 5 alkoxy, aldehydo, trifluoromethylthio, C1- 5 alkylsulphinyl, C1- 5 alkylsulphonyl, benzylthio, (C1- 5 alkyl) benzylthio, (C1- 5 alkoxy) benzylthio, halogenobenzylthio, mercapto, nitro, amino, di-(C1- 5 alkyl) amino, C1- 5 alkylamino, C1- 6 alkanoyloxy, mono-, di- or trifluoroacetoxy, benzyloxy, (C1- 5 alkyl) benzyloxy, (C1- 5 alkoxy) benzyloxy, and halogenobenzyloxy; R2 is H, C2- 5 alkenyl or C1- 5 alkyl; R3 is H, alkyl, alkenyl, or together with R13 an alkylidenyl radical or together with the carbon atom to which R3 and R13 are joined a cyclopropyl radical, otherwise R13 is H; R4 is H, C1- 5 alkoxy, fluorine, C1- 5 alkyl or trifluoromethyl; R5 is H or a C1- 5 alkyl, C1- 5 alkoxy, nitro, amino, mono- or di-(C1- 5 alkyl) amino, C1- 6 alkanoylamino, C1- 6 alkanoyl, bis-(hydroxy-C1- 5 alkyl) amino, 1-pyrrolidino, 4-methyl-1-piperazinyl, 4-morpholinyl, cyano, amino-C1- 5 alkyl, di - (C1- 5 alkyl) amino - C1- 5 alkyl, trifluoromethyl, halogen, di - (C1- 5 alkyl) sulphamoyl, benzylthio, (C1- 5 alkyl) benzylthio, (C1- 5 alkoxy) benzylthio, halogenobenzylthio, benzyloxy, (C1- 5 alkyl) benzyloxy, (C1- 5 alkoxy) benzyloxy, halogenobenzyloxy, C2- 5 alkenyl, C2- 5 alkenyloxy, 1 - aza - cyclopropyl, cyclopropyl (C1- 5 alkoxy) methyloxy, cyclobutyl (C1- 5 alkoxy) methyloxy, aryl, aryloxy, mercapto, haloalkyl, sulphamoyl, sulphoxide, carboxy or carboalkoxy group; are prepared by heating the corresponding acid with a carbodiimide.

Inventors

• 👤 Shen Tsung-Ying

Bibliographic Details