Synthesis and properties of 2-amino-4,6-dimethylnicotinic acid arylamides

It is shown that on boiling 2-amino-4,6-dimethylnicotinic acid arylamides with triethyl orthoformate in acetic anhydride, derivatives of 3-aryl-5,7-dimethyl-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidine are formed. The same compounds are obtained by ternary condensation of ethyl 2-amino-4,6-dimethylnicotinate with triethyl orthoformate and alrylamines. On reaction with urea or ammonium thiocyanate, the ethyl ester or anilides of 2-amino-4,6-dimethylnicothinic acid are converted to 2,4-dioxo- or 4-oxo-2-thio-pyrido[2,3-d]pyrimidines respectively.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1384–1386, October, 1992.     

Synthesis,structure, and properties of 2-[(4,6-di-tert-butyl-2,3-dihydroxyphenyl)thio]acetic acid amides

Russian Chemical Bulletin - New potential biologically active derivatives, in which the sterically hindered pyrocatechol moiety is linked through a 2-thioacetyl covalent bridge to a number of...     

Synthesis of substituted 2-aminoquinoline-3-carboxylic acid amides

Substituted 3-(2-nitrophenyl)-2-cyanoacrylic acid amides were synthesized by the Knoevenagel reaction and were then reduced with iron in acetic acid to the corresponding 2-aminoquinoline-3-carboxylic acid amides.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 11, pp. 1515–1517, November, 1988.     

Synthesis of nitroxylcarbamidophosphoric acid amides

A method for obtaining new organophosphorus nitroxyls was developed based on Kirsanov's phosphazo reaction.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 5, pp. 1139–1141, May, 1990.     

Synthesis of thiophosphoric acid amides

Conclusions The cyclohexylamido- and piperididothiophosphoric acids were obtained for the first time, and also piperazido-N,N-bisthiophosphoric acid as the Na and NH₄ salts.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 10, pp. 2402–2403, October, 1982.     

Synthesis of betulonic acid amides

Betulonic acid amides of interest as potential biologically active compounds were prepared. __________ Translated from Khimiya Prirodnykh Soedinenii, No. 3, pp. 259–264, May–June, 2008.     

Synthesis and conversions of 2-substituted cinchoninic acid amides

Amides of 2-oxo- or 2-thiocinchoninic acid have been obtained by the reaction of substituted amides of 2-chlorocinchoninic acid with sodium acetate or sodium sulfide. The reaction of 2-thiocinchoninic acid amides with hydrazine hydrate or ethyl cyanoacetate leads to derivatives of 2-hydrazinocinchoninic acid or (4-carbamoyl-2-quinolyl)cyanoacetic ester respectively, which were also obtained from 2-chlorocinchoninic acid amides.Perm Pharmaceutical Academy, Perm 614600. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 5, pp. 697–700, May, 1997.     

Synthesis of some esters and amides of 2-substituted 4,6-bis(p-carboxyphenoxy)-sym-triazine

A number of corresponding esters and amides were obtained by the reaction of the chlorides of 2-substituted 4,6-bis(p-carboxyphenoxy)-sym-triazines (CPT) with ethanol and some primary amines in the presence of a hydrogen chloride acceptor. It was observed that hydrazine and hydrazine hydrate have a cleavage effect on the C-O bond of chloride of CPT in the 4 and 6 positions even at 0 °C. Dihydrazides of CPT were synthesized at –40 °C.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1406–1411, October, 1981.     

Synthesis of benzimidazole-2-carboxylic acid amides from o-phenylenediamine and oxamic acid esters

A method for the preparation of N-R amides of benzimidazole-2-carboxylic acid on the basis of the reaction between o-phenylenediamine and esters of N-R oxamic acids was developed.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 5, pp. 684–686, May, 1982.     

Synthesis and functionalization of 4-arylamino-2-pyridone derivatives

New approaches to the synthesis of the previously unknown pyrimidine, 4-amino-2-pyridone, and 4-aminopyridine derivatives were developed based on the reactions of enaminoamides with dimethylformamide dimethyl acetal. New structural modifications of 4-amino-2-pyridone derivatives were performed. Numerous compounds of this type, which are of interest for biological studies, were prepared. Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 8, pp. 1421–1432, August, 2006.     

4,6-二甲基-2-取代嘧啶的合成

采用改进的合成方法以乙酰丙酮分别与胍、硫脲、脲反应合成了三种2位杂原子取代的嘧啶类化合物,收率83．8％-98．6％,其结构经1^H NMR,IR和MS表征。     

5-芳胺-6-氯-2, 3-二氰吡嗪的合成

本文以丙二腈为起始原料, 经过六步合成了中间体7, 化合物7和芳胺发生单取代得到目标产物5-芳胺-6-氯-2, 3-二氰吡嗪(8), 所合成的这10个目标产物文献上未见报道的, 通过了元素分析, IR, 1HNMR, MS证实其结构。粉末法测试表明它们都具有一定的二阶倍频效应。     

Synthesis and structure of 5,5-dialkyl-3-arylamino-2-thiohydantoins

The reaction of arylhydrazides of -alkyl--chlorocarboxylic acids with thiocyanate ions gave intermediate thiocyanates which rearranged to isothiocyanates on heating and the latter cyclized to 5,5-dialkyl-3-arylamino-2-thiohydantoins.Institute of Technical Chemistry, Urals Branch, Russian Academy of Sciences, Perm' 614000. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 898–903, July, 1997.     

Synthesis of new betulonic and oleanonic acid amides

Amides of betulonic and oleanonic acids with diethylenetriamine, triethylenetetramine, and spermidine were synthesized. Antitumor activity in vitro was not found for the conjugate of betulonic acid with diethylenetriamine.     

Synthesis based on furancarboxylic acid amides. 2. Synthesis of diamides of the furan series

The corresponding furancarboxylic acid diamides were obtained by the addition of primary amides of furancarboxylic acids to the double bond of vinyl butyl ether and the carbonyl group of various aldehydes..See [2] for Communication 1.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1316–1318, October, 1990.     

Synthesis of 2-methyl-4,6-diarylpyrilium tetrafluoroborates

Condensation of acetophenones with acetic anhydride in the presence of boron trifluoride etherate has given some 2-methyl -4,6-diarylpyrilium tetrafluoroborates. The optimum conditions for the synthesis of 2-methyl-substituted pyrilium salts have been established.Translated from Khimiya Geterotsiklicheskikh Soedenii, No. 2, pp. 173–176, February, 1985.     

Synthesis and antimicobacterial activity of 2-substituted 4-arylamino-6-methylpyrimidines

2-Substituted 4-arylamino-6-methylpyrimidines were synthesized by stepwise modification of the structure of 6-methyl-2-thiouracyl through the intermediate 2-(ar)alkylthio-6-methyl-4-chloropyrimidines. Some of the compounds synthesized exhibit expressed antimycobacterial activity.