Synthesis of 4,5-decamethyleneimidazole, 4,5-decamethyleneoxazole, 4,5-decamethyleneisoxazole, 4,5-decamethyleneimidazolone-2, and 4,5-decamethylenepyrazole from cyclododecanone derivatives

4,5-Decamethyleneimidazole, 4,5-decamethyleneoxazole, and 4,5-decamethyleneimidazolone-2 were synthesized by reactions of 2-bromocyclododecanone and 2-hydroxycyclododecanone with formamide, ammonium formate, and urea, respectively. Condensation of 2-formylcyclododecanone with hydroxylamine and hydrazine hydrate resulted in 4,5-decamethyleneisoxazole, and 4,5-decamethylenepyrazole, respectively.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 891–893, May, 1994.     

Synthesis of 2-aminomethyl derivatives of dihydrothiazolo[2,3-f]xanthine

2-Aminomethyl derivatives of dihydrothiazolo[2,3-f]xanthine were obtained by the reaction of 8-halo-7-(2,3-epithiopropyl)xanthines with amines.Fifteenth Anniversary of the All-Union Lenin Young Communist League Bashkir State Medical Institute, Ufa 450000. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 840–842, June, 1991.     

Synthesis and biological screening of 7-hydroxy-4-methyl-2H-chromen-2-one, 7-hydroxy-4,5-dimethyl-2H-chromen-2-one and their some derivatives

7-Hydroxy-4-methyl-2H-chromen-2-one (2), 7-hydroxy-4,5-dimethyl-2H-chromen-2-one (15) and their some derivatives were synthesized for exploring selected biological screening. The compounds 9 and 13 had shown high degree of cytotoxic activity. Three compound 9, 10 and 13 showed high degree of bactericidal activity amongst the present series.     

Synthesis of 2-carboxy-5,6-ethylenedioxyindole and its 3-, 4-, and 7-halo derivatives

A method for the synthesis of 2-carboxy-5,6-ethylenedioxyindole and its 4- and 7-chloro derivatives from 3,4-ethylenedioxyaniline and, correspondingly, its 2- and 5-chloro derivatives via the Fischer reaction was developed. It was established that in the case of bromination or chlorination under mild conditions 2-carbethoxy-5,6-ethylenedioxyindole forms 3-halo derivatives, while 5,6-ethylenedioxyindole itself forms only 3,7-dihalo derivatives. The closeness in the reactivities of the 3 and 7 ring positions of 5,6-ethylenedioxyindole (as compared with indole) is in agreement with the results of calculations of the quantum-chemical reactivity indexes for electrophilic substitution.Translated from Khimiya Geterotslklicheskikh Soedinenii, No. 9, pp. 1215–1219, September, 1982.     

Synthesis and membrane-protective activity of 4-aminomethyl derivatives of 2,6-diisobornylphenol

A series of 4-aminomethyl derivatives of 2,6-diisobornylphenol containing tertiary and secondary amino groups were synthesized. Their toxicity and the membrane-protective and antioxidant activity were assessed using red blood cells of laboratory mice as the test object. These compounds were shown to exhibit high membrane-protective and antioxidant activity, which substantially depends on the structure of the substituent and the concentration of the substance.     

Pteridines,LXXXIV. Synthesis,reactivity and properties of 1,3-dimethyllumazine-6- and 7-carboxaldehyde derivatives

Convenient syntheses of 1,3-dimethyllumazine-6- (7) and -7-carboxaldehyde ( 19 ) are described. The reactivity of the carboxaldehyde group has been investigated by oxidations, reductions and various carbonyl reactions forming a series of new derivatives. The newly synthesized compounds were characterized by elemental analysis, uv and ¹H-nmr spectra.     

Synthesis of 4-, 5-, 6-, and 7-azidotryptamines

Synthesis of azidotryptamines from commercially available nitroindoles via the corresponding amino tryptamines in good overall yields (15-38%) is presented.     

The 5,6- and 4,5-benzo derivatives of 1-hydroxy-7-azabenzotriazole

[structure: see text]. Syntheses of the two benzo derivatives of HOAt are described. Conversion of the two isomers to the corresponding onium-style coupling reagents gave in one case a guandinium species 14 and in the other, presumably as a result of steric factors, a uronium species 15. The two systems are compared as to their effectiveness in peptide coupling processes.     

Synthesis of 6- and 7-propargyloxy derivatives of 4-(3-fluoroanilino)-quinazoline

The preparation of the novel isomeric 6- and 7-propargyloxy derivatives of 4-(3-fluoroanilino)-quinazoline was achieved using a six-step process. An alternate method to the 7-propargyloxy derivative and analogous 7-propargyloxy containing compounds is also described.     

6-萘氧甲基-[1,3]二氧戊环并[4,5-g]喹啉-7-甲酸衍生物的合成（英文）

介绍了通过6-氯甲基-[1,3]二氧戊环并[4,5-g]喹啉-7-甲酸乙酯与1-和2-萘酚的Williamson醚合成反应及其随后的酯水解反应,"一锅法"高收率的合成了结构新颖的含有萘环结构的喹啉化合物,即2-(萘氧甲基)喹啉-3-羧酸.这种新合成的化合物可以为开发有用的药物活性先导化合物提供很好的底物.     

Synthesis of 4,5-diaryl-2-(n-methyl-3-carbazolyl)- and 4,5-diaryl-2-(n-methyl-1,2,3,4-tetrahydro-7-carbazolyl) imidazoyl radicals

A number of imidazoles were obtained by the reaction of substituted benzils with aldehydes of the carbazole series. Chlorobenzene solutions of the imidazoles take on a green coloration on oxidation with lead dioxide. The presence of free radicals in these solutions is confirmed by the ESR spectra and by the reaction with hydroquinone, diphenylamine, carbazole, and ,-diphenyl--picrylhydrazine.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 11, pp. 1550–1551, November, 1971     

Synthesis and investigation of 2-(2-quinolyl)-5, 6-benzocinchoninic acid and its derivatives

2-(2-Quinolyl)- and 2-(4-phenyl-2-quinolyl)-5,6-benzocinchoninic acids were synthesized, and their derivatives were obtained and decarboxylated. The UV and IR spectra of the compounds were studied, and it was found that all of the new compounds form colored Cu(I) complexes.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 239–241, February, 1973.     

19F-19F Coupling constants in the azole series. Synthesis of 3,4-, 4,5-, and 3,5-difluoropyrazoles

Stepwise syntheses of difluoroazoles $\text{1}$, $\text{2}$, and $\text{3}$ have been performed. The J_FF coupling constants are reported for the first time. Surprisingly, no coupling between F₄ and F₅ is observed.     

6-烷基-7-亚胺基-2-硫代-2,3,6,7-四氢噻唑并[4,5-d]嘧啶的合成、晶体结构与生物活性

通过3-苯基-5-氰基-2-硫代-2,3-二氢-4-乙氧亚甲胺基噻唑(5)与伯胺反应, 经中间体甲脒关环, 合成了10种新的噻唑并[4,5-d]嘧啶类化合物6a～6j. 所有化合物的结构均经1H NMR, IR和元素分析进行了表征, 并且采用X射线单晶衍射分析方法进一步测定了化合物6i的结构. 初步的生物活性试验表明, 部分标题化合物具有一定的杀菌或除草活性.