When treated with difluorocarbene, which was generated from FSO2CF2CO2SiMe3 a 1,8-bis(dimethylamino)naphthalene catalyst, N-(thioacyl)amidines underwent [4 + 1] cycloaddition to afford the corresponding amino-substituted 5,5-difluorothiazolines. Both dehydrofluorination and Hofmann elimination/SN2?-type reaction sequence enabled aromatization of obtained products, affording 5-fluorothiazoles. T...

A facile three step synthesis of a group of N1,N5-bis[4-(5-alkyl-1,2,4-oxadiazol-3-yl)phenyl]glutaramides, N1,N5-bis[4-(1,2,4-oxadiazol-3-yl)phenyl]glutaramide and N1,N5-bis[4-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)phenyl]glutaramide is described. These products are designed to function as masked bis-amidine prodrugs of a promising N1,N5-bis[4-(N'-(carbamimidoyl)phenyl]glutaramide antifungal l...

This study demonstrates the first enantioselective synthesis of hydroxyalkyl- and aminoalkyl-substituted imidazoles, oxazoles, and thiazoles. The approach developed utilizes a highly effective one-pot reaction cascade that consists of either an organocatalytic epoxidation or aziridination of α,β-unsaturated aldehydes coupled with a [3+2]-annulation, in which amidines, ureas, or thioureas act as...

The title compound, 2C(17)H(20)N(2)O·CH(2)Cl(2), was obtained by N-oxidation of the parent formamidine with m-chloro-peroxy-benzoic acid (m-CPBA). This is the first use of the above-mentioned synthetic route for the preparation of hydroxy-amidines. The title compound crystallizes as a cyclic dimer resulting from the presence of O-H⋯O and N-H⋯N hydrogen bonds.

Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 by reaction with aromatic amines at room temperature in good to excellent yields. Imidate was prepared by treatment of equimolar quantities of triethyl orthoformate and diaminomaleonitrile in refluxing dioxane. All the compounds were characterized fully by ...

Silica sulfuric acid as an efficient and reusable heterogeneous catalyst has been used for the preparation of amidines 2 from formimidate 1 by reaction with aromatic amines at room temperature in good to excellent yields. Imidate was prepared by treatment of equimolar quantities of triethyl orthoformate and diaminomaleonitrile in refluxing dioxane. All the compounds were characterized fully by ...

In normal Amount Total Error of recovery Method plasma added found (%) Spectrophotometric 079 0-5 1*28 -3-4 1*0 0.4 1*41 +2-5 -1*0 1.0 1*96 -4.0 -0-82 0-7 1-53 +1*4 -0*82 1*2 2*18 -1*7 Photoelectric 076 0 5 1F24 -4 0 -1-03 0-4 1*43 +1'2 -1-03 1.0 2*0 -3*0 -0'84 0 7 1*56 +2-8 -0*84 1*2 2*01 -2.5 Roe & Kuether (1943) -0-72 0 5 1-2 -4 0 -1.0 0.4 1*4 0.0 -1.0 1.0 1*96 -4*0 -0*88 0*7 1*6 +2-8 -0*88 ...