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1

Green synthesis of pyrimidine derivative

Sonawane R. P.

International Letters of Chemistry, Physics and Astronomy

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2014

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Vol. 2

64-68

EN

The majority of the drugs on the market today are entirely chemically synthesized in the laboratory. Several scientists had synthesized dihydropyrimidine (DHPMs) derivatives showing a wide spectrum of biological actions as antibacterials, antivirals as well as antitumor agents. This activity is principally due to presence of steriogenic carbon C4 in their structure. The current investigation is study and synthesis of dihydropyrimidinones efficiently and in high yields under mild, solvent free and eco-friendly conditions by using “Grindstone Chemistry Technique” catalyzed by CuCl2•2H2O and Conc. HCl. The obtained products have been identified by comparison with spectral data & their melting points. The synthesis of DHPMs derivative involves a multicomponent reaction (aldehyde derivative, urea /thiourea and 1,3-dicarbonyl compounds) in presence of HCl / NH4Cl as a catalyst. 3,4-dihydropyrimidin-2-(1H)-ones was synthesized and characterized using IR. The melting points was obtained 203 °C.

2

Comparative Study of Chemical Synthesis of Pyrimidine Derivatives by Using Grindstone Chemistry Technique and Conventional Metod

Sonawane R. P.

International Letters of Chemistry, Physics and Astronomy

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2014

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Vol. 14, iss. 1

22--27

EN

The majority of the drugs on the market today are entirely chemically synthesized in the laboratory. Several scientists had synthesized dihydropyrimidine (DHPMs) derivatives showing a wide spectrum of biological actions as antibacterials, antivirals as well as antitumor agents. This activity is principally due to presence of steriogenic carbon C4 in their structure. The current investigation is comparative study of chemically synthesis of two DHPMs derivatives by Biginelli Reaction using conventional method and grindstone chemistry technique. The synthesis of DHPMs derivative involves a multicomponent reaction (aldehyde derivative, urea /thiourea and 1,3-dicarbonyl compounds) in presence of HCl / NH4Cl as a catalyst. Two derivative viz. 3,4-dihydropyrimidin-2-(1H)-ones and 3,4-dihydropyrimidin-2-(1H)-thiones were synthesized and characterized using IR. The melting points were obtained are 208 °C and 210 °C respectively. “Grindstone Chemistry Technique” catalyzed by CuCl2•2H2O and Conc. HCl. gave more yield, solvent free and ecofriendly. The obtained products have been identified by comparison with spectral data & their melting points. This study will help to develop easy protocol for the synthesis of many more DHPMs derivative with high field.

3

The chemistry and synthesis of 1H-indole-2,3-dione (Isatin) and its derivatives

Sonawane R.P., Tripathi R.R.

International Letters of Chemistry, Physics and Astronomy

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2013

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Vol. 7, iss. 1

30--36

EN

Isatins are synthetically versatile substrates, where they can be used for the synthesis of a large variety of heterocyclic compounds. In this, a convenient method has been developed for the conversion of Indoles into Isatins and some heterocyclic derivative were synthesised such as 5- nitro-1H-indole-2,3-dione, 2-methylquinoline-4-carboxylic acid which may be used as raw material for drug synthesis. The general process utilizes the effective method for synthesis of Isatin from Indole is bromination and oxidation with an N-bromosuccinimide-dimethyl sulfoxide reagent. The nitration of Isatin at C-5 takes place by using KNO3, conc. H2SO4, 2-methylquinoline-4-caboxylic acid are usually obtained from pfitzinger reaction.

4

Comparative study of chemical synthesis of dihydropyrimidine (DHPMS) derivatives by Biginelli Reaction using microwave irradiation and conventional method

Sonawane R.P.

International Letters of Chemistry, Physics and Astronomy

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2013

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Vol. 5

7-11

EN

The majority of the drugs on the market today are entirely chemically synthesized in the laboratory. Several scientists had synthesized dihydropyrimidine (DHPMs) derivatives showing a wide spectrum of biological actions as antibacterials, antivirals as well as antitumor agents. This activity is principally due to presence of steriogenic carbon C4 in their structure. The current investigation is comparative study of chemically synthesis of two DHPMs derivatives by Biginelli Reaction using microwave irradiation and conventional method. The synthesis of DHPMs derivative involves a multicomponent reaction (aldehyde derivative, urea /thiourea and 1,3-dicarbonyl compounds) in presence of HCl / NH4Cl as a catalyst. Two derivative viz. 3,4-dihydropyrimidin-2-(1H)-ones and 3,4-dihydropyrimidin-2-(1H)-thiones were synthesized and characterized using IR. The melting points were obtained are 203 °C and 211 °C respectively. Microwave irradiation was easy and gave more yield than conventional method. This study will help to develop easy protocol for the synthesis of many more DHPMs derivative with high yield.

5

An extraction of the Isatin from the Couroupita Guianesis (cannon ball tree) and A novel synthesis of the N,N'-(2-oxo-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazole]-3',5'-diyl]diacetamide from the Isatin

Tripathi R. R., Sonawane R. P.

International Letters of Chemistry, Physics and Astronomy

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2013

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Vol. 10, iss. 2

119-125

EN

Isatins are synthetically versatile substrates, where they can be used for the synthesis of a large variety of Isatins and heterocyclic compounds. In this, the isatin were extracted from the floral material of Couroupita guianesis commonly known as an Cannon ball tree. After that, a novel heterocyclic spiro derivative having an IUPAC name N,N’-(2-oxo-3’H-spiro[indoline-3,2’-[1,3,4] thiadiazole]-3’5’-diyl)diacetamide were synthesized , which may be used as raw material for drug synthesis. A spiro compound N,N’-(2-oxo-3’H-spiro[indoline-3,2’-[1,3,4] thiadiazole]-3’5’-diyl)diacetamide were synthesise by refluxing Isatin And thiosemicarbazone in ethanol and then on heating with acetic anhydride underwent to cyclization into intermediate that on acetylation of the NH and NH2 groups afforded the spiro compound.