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1.
The reaction of 4-(amino-substituted)-2-methylthio-6-chloropyrimidine-5-carbonitriles with hydrazine and methylhydrazine was used to synthesize 3, 4-diamino-6-methylthio-1H-pyrazolo[3, 4-d]pyrimidines. It was shown that the formation of pyrazolopyrimidines proceeds through intermediate 6-hydrazinopyrimidine-5-carbonitriles.Department of Organic Chemistry, Vil'nyus University, Vil'nyus 2006. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 831–836, June, 1996. Original article submitted February 9, 1996.  相似文献   

2.
A number of substituted 2H-pyrazolo[3,4-d]pyridazines, pyridazin-7(6H)ones, and -pyrid-azine-4,7(5H,6H)diones have been prepared from the 3,4-diacyl-, 3-carbethoxy-4-acyl-, 3-carbethoxy-4-cyano-, and 3,4-dicarbethoxy-pyrazole derivatives and hydrazine hydrate. The structures of the compounds prepared were inferred from their elemental analyses and spectral data. On the basis of spectroscopic data it was concluded that pyrazolopyridazinones have the oxo form, whereas the monohydroxymono oxo structure is preferred for pyrazolopyridazine-diones.  相似文献   

3.
谢君  马月龙  肖元晶  杨琍苹 《有机化学》2004,24(11):1436-1439
用固相合成技术合成了吡唑并[5,4-d]嘧啶的一类衍生物8.以Merrifield树脂为原料,与化合物3反应得到树脂4.4经过还原胺化、取代、分子内亲核加成反应得到树脂7,再由三氟醋酸断裂得到化合物3,4-二胺-1H-吡唑并[5,4-d]嘧啶.  相似文献   

4.
5.
Starting from the readily available 4-bromomethyl-5-benzoyl-1,2,3-thiadiazole and 5-bromomethyl-4-benzoyl-1,2,3-thiadiazole; thieno[3,4-d][1,2,3]thiadiazole, selenolo[3,4-d][1,2,3]-thiadiazole and pyrrolo[3,4-d][1,2,3]thiadiazole were synthesized in good yield.  相似文献   

6.
The imidazo[4,5-d]-1,2,3-triazine and pyrazolo[3,4-d]-1,2,3-triazine analogues of the potent anticonvul-sant purine, BW 78U79 (9-(2-fluorobenzyl)-6-methylamino-9H-purine, 1 ), were synthesized and tested for anticonvulsant activity. The imidazo[4,5-d]-1,2,3-triazines 11–13 were prepared in four steps from 5-aminoimidazole-4-carboxamide (2) and the pyrazolo[3,4-d]-1,2,3-triazines 18–21 were synthesized starting with 5-amino-1-(2-fluorobenzyl)pyrazole-4-carbonitrile (14) . The intermediate 1,2,3-triazin-4-ones 6 and 16 were converted to the 4-substituted targets via the 4-(4-dimethylaminopyridinium) salts 10 and 17 . Imidazotriazine 11 had potent anticonvulsant activity against maximal electroshock-induced seizures, but its propensity to cause emesis precluded further development.  相似文献   

7.
New androsteno[17,16-d]pyrazoles and -pyrazolines with pyrazolo[3,4-d]pyrimidine fragments were synthesized. A reaction of 3β-hydroxypregna-5,16-dien-20-one and its 3-O-acetyl derivative with 6-hydrazino-3,4-dimethyl-1H-pyrazolo[3,4-d]pyrimidine led to hydrazones at position 20 of the pregnenolone molecule, a possibility of their cyclization was studied. Upon melting, the hydrazones cyclize with the formation of pyrazoline ring annulated with ring D of the steroid at positions 16 and 17. Reflux of the hydrazones in mesitylene with AcOH leads to a mixture of two reaction products: androsteno[17,16-d]pyrazole and a dodecahydro-13H-phenanthro[1′,2′:5,6]pyrano[2,3-d]pyrazole derivative. Apparently, this transformation proceeds through the corresponding epoxide with subsequent rearrangement, which leads to the ring D expansion.  相似文献   

8.
Starting from the readily available 4-bromomethy-5-carbethoxy 1,2,3-thiadiazole (V), 5-bromomethy-4-carbethoxy-1,2,3-thiadiazole (IX) and ethyl 2-aryl-5-bromomethyloxazole-4-carboxylate (XIV), 4,10-dihydro-10-oxo[1]benzoxepino[3,4-d][1,2,3]thiadiazole (Ia), 4,10-dihydro-10-oxo[1]benzothiepino[3,4-d][1,2,3]thiadiazole (Ib), 4,10-dihydro-4-oxo[1]benzothiepino[4,3-d] [1,2,3]thiazole (II), 2-aryl-4,10-dihydro-4-oxo[1]benzoxepino[4,3-d]oxazoles (XIXa-XIXc) and 2-aryl-4,10-dihydro-4-oxo[1]benzothiepino[4,3-d]oxazoles (XIXd-XIXf) were prepared.  相似文献   

9.
The synthesis and characterization of a number of 3-aryl-6H-isoxazolo[3,4-d]pyrazolo[3,4-b]pyridines and 3-aryl-6H-isoxazolo[5,4-d]pyrazolo[3,4–6]pyridines from common precursors, 5-benzoyl-4-chloro-1H-pyrazolo-[3,4-b]pyridines, has been described. The structures were determined by unambiguous chemical synthesis and by isolation and 13C nmr analysis of some key, isolated, intermediates. The ability of these compounds to displace [3H]flunitrazepam from CNS binding sites was also observed.  相似文献   

10.
The synthesis of the parent ring system and some of the derivatives of 1H-pyrazolo[3,4-d]thieno[2,3-b]pyridine are described.  相似文献   

11.
3-Hydrazino-7-methyl-5-phenyl-5H-pyrazolo[3,4-c]-as-triazine 1 underwent ring closure and/or condensation reaction with formic acid, acetic acid, acetic anhydride and benzoyl chloride to afford 1H-pyrazolo-[3,4-d]-s-triazolo[3,4-c]-as-triazines 2, 5 and 7a and/or N-acyl derivatives 3, 4 and 6 . N-Acyl derivatives 3 and 6 underwent cyclisation reaction on treatment with phosphoryl chloride to give 5 and 7a . 3-Methyl-1-phenyl-8-aryl-1H-pyrazolo[3,4-e]-s-triazolo[34,-c]-as-triazines 7 were also prepared by the reaction of the hydrazono derivatives 8 wit thionyl chloride. On treatment of 1 with nitrous acid gave the 8H-pyrazolo[3,4-e]tetrazolo-[5,1-c]-as-triazine 9 . Compound 1 underwent ring closure with carbon disulphide or ethyl chloroformate to 1,7-dihydro-8H-pyrazolo[3,4-e]-s-triazolo[3,4-c]-as-triazine derivatives 10 and 12 . Reaction of 1 with ethyl acetoacetate or acetylacetone gave 3-pyrazolo derivatives 13 and 14 .  相似文献   

12.
为了发现新型的原卟啉原氧化酶抑制剂, 根据生物合理设计方法, 设计并合成了一系列的结构新颖的3H-吡唑并[3,4-d][1,2,3]三嗪-4-酮衍生物. 利用不同取代的5-氨基-吡唑-4-甲酰氯与取代苯胺反应制得的5-氨基-N-苯基-1H-吡 唑-4-甲酰胺衍生物, 经进一步重氮化得到目标化合物, 并对化合物3f进行衍生化. 所得目标化合物的结构均经1H NMR, IR和元素分析确证. 生物活性测定结果表明, 部分化合物对原卟啉原氧化酶有较高的抑制活性, 讨论了其结构与活性的关系.  相似文献   

13.
为了发现新型的原卟啉原氧化酶抑制剂,根据生物合理设计方法,设计并合成了一系列的结构新颖的3H-吡唑并[3,4-d][1,2,3]三嗪-4-酮衍生物.利用不同取代的5-氨基-吡唑-4-甲酰氯与取代苯胺反应制得的5-氨基-N-苯基-1H-吡唑-4-甲酰胺衍生物,经进一步重氮化得到目标化合物,并对化合物3f进行衍生化.所得目标化合物的结构均经1HNMR,IR和元素分析确证.生物活性测定结果表明,部分化合物对原卟啉原氧化酶有较高的抑制活性,讨论了其结构与活性的关系.  相似文献   

14.
Russian Chemical Bulletin - Reactions of pyrazolo[3,4-d]pyrimidine-containing hydrazines with pregnenolone derivatives were studied. The reaction of...  相似文献   

15.
Conclusions We synthesized the cis-3- and 4-methyl-2-oxo-6-(-carboxybutyl) hexahydro [3,4-d]-imidazoles by the reduction of the 3- and 4-methyl-2-oxo-2,3-dihydro-6-(carboxybutyl)-1H-thieno [3,4-d] imidazoles with HSiEt3 in CF3COOH and subsequent alkaline hydrolysis of the intermediate methyl ethers.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 7, pp. 1634–1636, July, 1980.The authors express their gratitude to Prof. A. Mark (France) for supplying the sample of 2-oxo-4-methyl-6-(6-carboxybutyl)hexahydrothieno[3,4-d]imidazole.  相似文献   

16.
The selenium dioxide oxidation of a series of 1,2,3,4-tetrahydrophenanthrone and 1,2,3,4-tetrahydrophenanthren-4-one semicarbazones afforded 4,5-dihydrophenanthro[4,3-d]-1,2,3-selenadiazoles and 10,11-dihydrophenanthro[1,2-d]-1,2,3-selenadiazoles. The latter series which represent a new type of selenaazasteroidal compounds were pyrolyzed and gave the corresponding 1,4-deselenine derivatives.  相似文献   

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20.
A new synthesis of 4-methoxy (or ethoxy)-1,6-diaryl-1H-pyrazolo[3,4-d]pyrimidine derivatives is described. An efficient one-step methodology for the title compounds was achieved by using 5-amino-1-aryl-1H-pyrazole-4-carbonitriles with arylaldehydes in CH3OH or C2H5OH and NaOH at 60 °C. The new compounds were obtained in moderate to good yields as stable solids and easily purified by filtration.  相似文献   

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