含氮杂环三烃基锡衍生物的合成及其生物活性

本文合成了14个含氮杂环三烃基锡衍生物,红外光谱,核磁共振谱和质谱的研究表明三烃基锡-1,2,4-三氮唑为以氮原子作桥联的五配位聚合结构化合物,化合物的生物活性和生物选择性主要取决于锡原子上的三烃基。     

SYNTHESIS,REACTIONS AND BIOLOGICAL ACTIVITY OF PHOSPHORUS-CONTAINING DERIVATIVES OF CHROMONE AND COUMARIN

Chromone and coumarin derivatives exhibit a wide spectrum of biological activity, including spasmolytic, antiarrhythmic, cardiothonic, antiviral, and anticancer properties. Phosphorus-containing chromone and coumarin derivatives form a novel group of compounds, possessing remarkable cytotoxicity and alkylating and anticancer activity against selected tumor cell lines. Derivatives containing a phosphorus atom at position 2 of a γ-pyrone ring are known to be efficient antibacterial agents.

This review presents methods developed for the synthesis of derivatives of chromone and coumarin that contain a phosphonate moiety. Among them, the reaction of derivatives of 2-hydroxyacetophenone with phosphonic compounds is the one most frequently used. Some analogues were characterized by X-ray crystallography.     

SYNTHESIS AND APPLICATION OF SOME NEW 5-SULPHONYL-N-HETEROCYCLO-8-HYDROXYQUINOLINE DERIVATIVES AS POTENTIAL DRUGS

Abstract

Some new sulphonyl-N-heterocyclo-8-hydroxy quinolines have been synthesised by the reaction of 8-hydroxyquinoline-5-sulphonyl hydrazide with different active methylene compounds. The pyrazole, pyrazoline, pyrazolidine and pyridazine derivatives were reacted with some metal cations to give the corresponding chelates. All synthesized compounds have been screened in vitro for their biological activities.     

THE BEHAVIOR OF N-PHENYLIMINOPHOSPHORANE TOWARDS o- AND p-QUINONES. NEW SYNTHESIS OF DIOXAZOLE AND OXADIAZOLE DERIVATIVES

ABSTRACT

N-Phenyliminophosphorane (1) reacts with 9,10-phenanthrenequinone (2a) to give the new products 2-phenylphenanthro[9,10-d][1,3,2]dioxazole (4a) and (10Z)-10-(phenylimino)-9(10H) phenanthrenone (4b). The reaction of 1 with 1,2-naphthoquinone (2b) afforded both the dioxazole derivative 5a and the known 2-anilino-naphthoquinone-1,4-anil (5b). On the other hand, 2,6-di-tert-butyl-2,3-diphenyl-2,3-dihydro-1,2,3-benzoxadiazole (6) was obtained from the reaction of (2c) with phosphinimine (1). Application of reagent 1 on 2d and 2e renders (6E)-2,3,4,5-tetrahalogeno-6-(phenylimino)-2,4-cyclohexadien-1-one 7a and 7b, respectively. Moreover, p-quinones (3a–3c) react with phosphinimine (1) to yield products 8, 9 and 10, respectively. Mechanisms accounting for the formation of the new products are discussed and the probable structures of the products are presented based on analytical and spectroscopic data.     

STUDIES ON THIAZOLOPYRIDINES. PART 5: SYNTHESIS OF HITHERTO UNKNOWN THIAZOLINONE AND THIAZOLO[3,2-a]PYRIDINE DERIVATIVES HAVING IN THEIR STRUCTURE THE MORPHOLIN-4-YL MOIETY

Condensation of thiazolinone 1 with benzaldehydes 2a, b in ethanolic piperidine afforded the methylidene derivatives 3a, b. Cyclocondensation of compound 3b with malononitrile furnished the novel thiazolo[3,2-a]-pyridine 5. Also, compound 3b was condensed with dimethylformamide-dimethylacetal (DMF-DMA) and triethylortho-formate to yield N,N-dimethylamino 6 and ethoxymethylene 7 derivatives respectively. The novel thiazolo[3,2-a]pyridines 10a, b were obtained by cyclocondensation of compounds 3a, b with benzylidene-malononitriles 8a, b. Similarly, cyclocondensation of compound 3b with benzylidenemalononitrile 11 afforded the thiazolopyridines 12a–c. Ternary condensation of compound (12), 4-morpholinobenzaldehyde 2b and malononitrile (1:1:1 molar ratio) produced the thiazolopyridines 14a–c. When compound 10b was subjected to react with malononitrile in dioxane/piperidine under reflux the novel condensed heterocyclic system 18 was obtained. Treatment of ortho-aminocarbonitrile 10b with formic acid, aromatic aldehyde and triethylorthoformate furnished the thiazolo[2′,3′:1,6] pyrido[2,3-d] pyrimidine 20, azomethine 21a, b and ethoxymethylene 22 derivatives respectively. The structure of the synthesized compounds was established by analytical and spectral data.     

以硫醚为主链的螯合树脂研究Ⅰ.4-氨基安替吡啉树脂和乙基原磺酸基树脂的合成及吸附性能

聚环硫氯丙烷或环硫氯丙烷与环氧氯丙烷共聚物，在少量二乙烯三胺存在下制得交联预聚物，将交联预聚物与4－氨基安替吡啉（4AAP）或乙基原磺酸钾（PEA）反应，制得四种侧链带氨基安替吡啉，乙基原碘酸基的新型螯合树脂。它们对贵金属具有优良的吸附性能和高的吸附选择性。并通过X－射线光电子能谱初步探讨了树脂对金属离子的螯合作用。     

稠杂环化合物的研究 Ⅵ.3—（3‘—吡啶基）—6—脂肪基／芳香基均三唑并[3,4—…

本文研究了３－（３＇－吡啶基）－４－氨基－５－巯基－１，２，４－三唑在ＰＯＣｌ３存在下与脂肪酸和芳香酸的缩合反应，制得２４种新的３－（３＇－吡啶基）－６－脂肪基／芳基均三唑并［３，４－ｂ］－１，３，４－噻二唑，利用元素分析、ＩＲ、＾１Ｈ ＮＭＲ及ＭＳ方法确认了结构。部分化合物进行了抗菌和除草试验。     

Me4Bzo2[14]六烯(2-)N4金属配合物的结构和反应性研究 Ⅰ.溴碘加成物的合成和振动光谱研究

本文合成了Co(Ⅱ)、Ni(Ⅱ)、Cu(Ⅱ)、Cu(Ⅱ)大环配合物及其溴碘加成物,研究了远红外和Raman光谱,对MN₄局部进行了伸缩振动的简正坐标分析,求得了各化合物的键角和伸缩力常.通过Raman光谱初步确定了溴碘的存在形式.对溴碘加成物的叠层结构和各化合物的成键进行了讨论.