Search

Novel benzamide derivatives, N-[1-(aminocarbonyl)-2-(1-piperidinyl)ethyl]benzamides (4 and 5), were prepared from the reaction of beta-piperidinoalanine (6) as the starting material.

New oxazolidin-2-ones (3), which mimic the clinically useful antibacterial agent (1) (Linezolid) were prepared by using a cyclization procedure with diethyl carbonate from aminoalcohol (7) starting with DL-serine methyl ester hydrochloride (4) and aromatic carboxylic acid derivatives (5).

A nucleophilic addition of phenol to N-(2-pyridylmethylene) aniline (I) is described. Electron density around carbon atom ortho to phenolic hydroxyl group and acidity of phenol are the two factors governing the outcome of the reaction. The effects of structural variation of Schiff base on its reactivity are also discussed. Extension of the reaction involved addition of 8-hydroxyquinoline to the Schiff base (I).

A new method for the syntheses of 1, 2-dipyridylethylene and its derivatives is described. The method involves condensation between N-oxides of picoline, lutidine, and quinaldine and pyridinemethanol in the presence of potassium hydroxide. Some stilbazole syntheses were also described.

A new synthesis of N-(2-pyridylmethylene) aniline (I) is described. The method consists of heating a mixture of 2-pyridinemethanol, aniline, and nitrobenzene in the presence of potassium hydroxide. Extension of the reaction to some related compounds was made. By-products accompanied with ortho-substituted derivatives of I were characterized as pyridylmethylene-bis-amines.

A new method for the synthesis of 5-substituted perhydroazocines and related compounds is described. The method consists of the C(7a)–N(4) bond cleavage of quaternary ammonium salts of 7a-substituted hexahydropyrrolizines which are easily prepared from 1,2,3,5,6,7-hexahydropyrrolizinylium perchlorate.

A new synthesis of 4H-1,4-benzothiazines, consisting of the condensation of o-aminobenzenethiol with cyclohexane-1,3-diones, acetylacetone, benzoylacetone, or ethyl acetoacetate in dimethyl sulphoxide, is described. An oxidative cyclisation mechanism, involving an intramolecular nucleophilic attack in an intermediate enaminoketone, is suggested.