A. N. Kost

Synthesis of substituted pyridinecarboxylic acids and study of their properties

A series of substituted pyridinecarboxylic acids and their N-oxides has been synthesized, their dissociation constants and electrophoretic mobility have been measured, and their pharmacological action has been studied. The presence of a satisfactory correlation between the pKa of of 4-substituted pyridinecarboxylic acids or their oxides and the σp electronegativity constants of the substituents has been shown. A linear dependence between dissociation constants and electrophoretic mobility of pyridinecarboxylic acids or their N-oxides has been found in various buffer solutions. The pharmacological action of a number of the synthesized compounds has been studied.

O-benzyl-N-(2-indolyl) urethans

The cancero ly t ic act ivi ty [1,2] and anesthetic effect of urethans [3] a re known, but only isolated examples of N-he te roy lure thans were subjects for study. Thus, de r iva t ives of pyridine containing a ca rbamic acid grouping act as psychotropic media [4], and quinolylurethans have an ant imetabol ic effect on glutamic dehydrogenase [5]. Inhibitors of cho l ines te rase [6] a re known among analogous compounds of the indole s e r i e s .

Synthesis of fusaric acid and its analogs

Summary1. A new method for synthesizing fusaric acid and its analogs has been proposed which starts from 2-methyl-5-ethynylpyridine; this is alkylated and the hydrogenated 2-methyl-5-alkynylpyridines are oxidized to the corresponding 5-alkylpicolinic acids.2. The mass-spectroscopic behavior of the 2-methyl-5-alkylpyridines has been studied.

Use of kovats indices for identifying sex pheromones

The gas-chromatographic retention indices of a number of unsaturated alcohols and their acetates and unsaturated expoxides on two phases of different polarities have been determined.The tabular results obtained used have been used to determine the lengths of the chains and the functionalities of the sex pheromones of two species of mothMamestra brassicae L. andMarnestra oleracia L.

Phthalazine and related heterocycles

ConclusionsEsters of 3-substituted 4-phthazthione-1-carboxylic acids were synthesized by the reaction of the corresponding oxygen analogs with phosphorus pentasulfide. 4-alkylthiophthalazine-1-carboxylic acids and their derivatives were obtained by alkylation. From UV spectra, it was concluded that the potentially tautomeric compounds had the thione structure.

Phthalazine and heterocycles related to it

ConclusionThe synthesis of a number of dialkylaminoalkyl esters and the corresponding amides of 4-phthalazone-1-carboxylic acids has been described. Some of these compounds possess local anaesthetic and short-term hypotensive activity.

Synthesis of 5-hydroxyalkynylpicolinic acids

A method for the selective oxidation of 2-methyl-5-ethynyl-and 2-methyl-5-hydroxyalkynylpyridines to the corresponding 5-substituted picolinic acids without affecting the acetylenic bond and the carbonyl group has been developed.

The formation of symmetrical diaminoketones by the action of acetic anhydride on acetyl-N-methylamino acids

SummaryWhen acetyl-N-methylamino acids are heated with acetic anhydride, bis-acetyl derivatives of N,N′-dimethyl-α, α′-diaminoketones are formed.

The action of acetic anhydride on N-methyltryptophans

SummaryDepending on the reaction conditions, acetylation of the methylamino acid dl-abrine and 5-methoxy-dl-abrine gives acetylamino acids, acetyl dipeptides, and more complex compounds of the peptide type.