A series of new N-acyl-substituted derivatives of the physiologically active alkaloid anabasine were synthesized and described. Their compositions and structures were identified using IR and 1 H NMR spectroscopy. These compounds were found to have moderate antibacterial and antifungal activities.

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Thiazolo[3,2-a]pyrimidines were obtained in good yield by the reaction of 4-aryl-substituted 3,4-dihydropyrimidine(1H)-2-thiones and methyl chloroacetate in boiling toluene. Their structures were shown by 1 H NMR spectroscopy and X-ray crystallography.Recently there has been a considerable growth in the number of publications on the chemistry of 4-aryl-3,4-dihydropyrimidin-2-ones and 4-aryl-3,4-dihydropyrimidine-2-thiones obtained by three-component condensation in the Biginelli reaction is associated with the displaying by these readily available compounds a wide range of pharmacological activities -analgesic, antibacterial, antihypertensive, etc. [1-3]. The attention of synthetic chemists was drawn to the presence in 4-aryl-3,4-dihydropyrimidine-2-thiones of several reactive nucleophilic centers allowing for a variety of mono-and dialkylation, acylation [4][5][6], and also the very prospective cyclization reaction. For example, the conversion of 4-phenyl-3,4-dihydropyrimidine(1H)-2-thione into 3,5-dihydro-2H-thiazolo[3,2-a]pyrimidine by boiling it in DMF with chloroacetic acid has been described [7]. Attempts to carry out analogous cyclizations with 4-methoxy-and 2,4-dimethoxyphenyl-substituted 3,4-dihydropyrimidine(1H)-2-thiones gave rise to considerable amounts brightly colored by-products, difficult to separate from the desired product.

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Keywords: methacryloylthiosemicarbazide of isonicotinic acid, intramolecular heterocyclization, X-ray crystallography.Previously the synthesis was reported of β-N-(methacryloylcarbamothioyl)isonicotinohydrazide (1) which, on boiling in 2-propanol for 10-16 h, underwent intramolecular cyclization to give β-N-(5-methyl-4-oxo-5,6-dihydro-4H-1,3-thiazin-2-yl)isonicotinohydrazide (2) [1]. The objective of the present work includes the study of the reaction of thiosemicarbazide 1 with a series of amines with the aim of obtaining the corresponding products of nucleophilic addition at the activated C=C bond.However mixing compound 1 with equimolar quantities of cyclic secondary amines (morpholine, piperidine) or alkaloids (anabasine, cytosine) in ethanol or 2-propanol solutions at about 30°C gave not the expected addition products 3 but the product of heterocyclization of compound 1 -the substituted 5,6-dihydro-1,3-thiazin-4-one 2 in 82% yield. Under these conditions cyclization of compound 1 occurred considerably faster (~1 h) than the same reaction in boiling 2-propanol reported previously [1]. The yield of product 2 did not depend on either the structure or the basicity of the amine and alkaloid starting materials.It is probable that the presence of base in the reaction medium facilitates the formation of the thiol form of compound 1 which is necessary for its cyclization. The 1 H NMR and IR spectra of samples of compound 2 obtained by using various amines or on boiling in 2-propanol [1] were identical.