Abstract

Novel 1,3-cyclopentathiazine and pyrimidothiazine derivatives were synthesized starting from 7-benzyl-4-phenylcyclopenta[d][1,3]thiazin-2-amine (CTA) prepared by a one-pot multicomponent reaction of cyclopentanone, benzaldehyde, and thiourea. Cyclocondensation of CTA with benzylidenemalononitrile gave a pyrimidothiazine. Oxidation of cyclopentathiazine with hydrogen peroxide afforded the corresponding epoxide, while its alkylation with ethyl iodide yielded an N-ethyl derivative. Cyclopentylidenemalononitrile was reacted with formaline and carbon disulfide to obtain pyridine-4-carbonitrile and thiapyrane, respectively, and the reactions of cyclopentylidenemalononitrile with aryl isocyanate and aryl isothiocyanate gave condensed diimino-substituted cyclopentanaphthyridine-1,6-dione and dithiaacenaphthylene-3,8-diylidedibenzamide, respectively. Heating cyclopentanone with benzoyl isothiocyanate and benzoyl chloride produced a sulfide derivative and an enolic dione, respectively. The structures of the newly synthesized compounds were confirmed by spectral analysis, and some products were screened for anticancer activity.

中文翻译：

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1,3-环戊噻嗪和嘧啶并噻嗪衍生物的一锅多组分合成及其抗癌活性

摘要

从7-苄基-4-苯基环戊达[ d ] [1,3]噻嗪-2-胺（CTA）开始，通过环戊酮，苯甲醛和苯甲醛的一锅多组分反应合成了新的1,3-环戊噻嗪和嘧啶噻嗪衍生物。硫脲。CTA与亚苄基丙二腈的环缩合反应得到嘧啶并噻嗪。用过氧化氢氧化环戊噻嗪得到相应的环氧化物，而用碘乙烷烷基化则得到N-乙基衍生物。使环戊二烯丙二腈与福尔马林和二硫化碳反应，分别得到吡啶-4-甲腈和噻喃，然后将环戊二烯丙二腈与异氰酸芳基酯和异硫氰酸芳基酯反应，得到缩合的二亚氨基取代的环戊萘吡啶-1,6-二酮和二噻吩并8啶基二环二苯甲酰胺。将环戊酮与异硫氰酸苯甲酰酯和苯甲酰氯一起加热，分别制得硫化物衍生物和烯醇二酮。通过光谱分析证实了新合成化合物的结构，并筛选了一些产品的抗癌活性。