G. A. Suboch

New Synthesis of Diethyl-5-[(N,N-Diethylglycyl)Amino]-2-Hydroxy-4,6-Dimethylisophthalate

A new convenient synthesis of diethyl-5-[(N,N-diethylglycyl)amino]-2-hydroxy-4,6-dimethylisophthalate with anti-arrhythmic properties was developed.

Oxidative synthesis ofpara-nitrophenol derivatives

As is known, para-nitrophenol and its halogen-substituted derivatives exhibit antifungal properties; the maximum activity was reported for 2-chloro-4-nitrophenol (I) [1]. Compound I enters into the composition of the antimycotic preparation nitrofungin (SPOFA, Czech Republic). To date, compound I has been obtained either by chlorinating 4-nitrophenol with free chlorine in acetic acid, with the chlorine absorption monitored by weight [2], or by chlorinating a 4-nitrophenol emulsion in a dilute hydrochloric acid at a temperature above the melting point of 4-nitrophenol [3], or by chlorinating 4-nitrophenol in sulfuric acid [4]. As seen, all these methods involve the use of free gaseous chlorine. In the course of works devoted to creation of a domestic antimycotic preparation, we have studied the possibility of obtaining compound I using a more convenient technology. The idea was based on the fact that the action of some oxidizers upon hydrochloric acid is accompanied by the evolution of chlorine. The most readily available and convenient of these oxidizing agents is hydrogen peroxide.

Synthesis of nitrosopyridinols by cyclocondensation of isonitroso β-dicarbonyl compounds with cyanoacetamide

The cyclocondensation of isonitroso β-dicarbonyl compounds with cyanoacetamide leads to nitroso derivatives of the pyridine series. The corresponding nitrosopyridinols are formed when isonitroso β-diketones participate in the cyclization, while nitrosopyridinediols are formed from isonitroso derivatives of β-oxo carboxylic acid esters.