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Shinde G.B.,A.P.Pharma | Niphade N.C.,A.P.Pharma | Deshmukh S.P.,A.P.Pharma | Toche R.B.,Organic Chemistry Research Center | Mathad V.T.,A.P.Pharma
Organic Process Research and Development | Year: 2011

Described is a new, practical, and one-pot process, based on the Forster reaction, for the synthesis of cinacalcet hydrochloride (1), a calcimimetic agent and calcium-sensing receptor antagonist. The synthesis comprises the condensation of (1R)-(+)-1-naphthylethyl amine (2) with benzaldehyde (3) followed by reaction of obtained Schiff's base 4 with 1-(3-halopropyl)-3- (trifluoromethyl)benzene (5) to provide highly unstable iminium salt 6. Subsequent hydrolysis of 6 with water in the same pot yielded cinacalcet. The treatment of cinacalcet with hydrochloric acid during the workup process furnished 1 with an overall yield of around 60%. Our synthetic approach for 1, discussed in this report demonstrates industrial application of the century-old, unexplored name reaction, "Forster's Reaction" or Forster-Decker synthesis. © 2011 American Chemical Society. Source


Chikhalikar S.,Bharatiya Vidya Bhavans Nm Institute Of Science | Bhawe V.,Bharatiya Vidya Bhavans Nm Institute Of Science | Jachak M.,Organic Chemistry Research Center | Ghagare M.,Organic Chemistry Research Center
European Journal of Organic Chemistry | Year: 2011

Two alternative methods for the synthesis of biologically important pyridin-2(1H)-one derivatives have been developed. The behavior of enamine 1 with aromatic amines in an aqueous solution of HCl resulted in the formation of substituted enamines 2a-f at ambient temperature. The obtained product enamines 2a-f, upon treatment with 2,2,6-trimethyl-4H-1,3-dioxin-4-one, generated pyridin-2(1H)-one derivatives 5a-f along with the unwanted side products 8a-f. However, the exclusive formation of pyridin-2(1H)-one derivatives 5a-f was achieved when starting from β-enaminones 3a-f, which were synthesized successfully from enamine 1 and aromatic amines at elevated temperatures. Compounds 2 and 3 have been used as precursors in the synthesis of pyridin-2(1H)-one derivatives. Temperature-dependent reaction diversity was observed for enamine 1 and the exclusive formation of pyridin-2(1H)-one derivatives 5 was possible. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source


Toche R.B.,Organic Chemistry Research Center | Chavan S.N.,Organic Chemistry Research Center
Journal of Fluorescence | Year: 2014

4-Hetero-1-yl-2-bromothieno[3,2-c]pyridines 3(a-d) were synthesized by the reaction of 2-bromo-4-chlorothieno[3,2-c]pyridine (1) and cyclic amine 2(a-d), which on Suzuki coupling with substituted boronic acids 4(a-f) exclusively converted to corresponding 4-hetero -1-yl-2-arylthieno[3,2-c]pyridine 5(a-x) in good yields. The effect of donor-acceptor substituent on absorption emission properties and fluorescent quantum yield of new thienopyridine derivatives 5(a-x) were studied. © 2013 Springer Science+Business Media New York. Source


Chikhalikar S.,Bharatiya Vidya Bhavans Nm Institute Of Science | Bhawe V.,Bharatiya Vidya Bhavans Nm Institute Of Science | Ghotekar B.,Organic Chemistry Research Center | Jachak M.,Organic Chemistry Research Center | Ghagare M.,Organic Chemistry Research Center
Journal of Organic Chemistry | Year: 2011

The nucleophilic vinylic substitution reaction of the aliphatic enaminone 3-dimethylamino-2-formyl acrylonitrile 1 with the nucleophiles malononitrile and ethyl cyanoacetate produced the two unusual reaction adducts 3a and 3b in good to moderate yield under milder reaction conditions. Upon reaction with aromatic amines, these adducts yielded enamines 4 and 5, which eventually cyclized in the presence of base to produce the novel pyridin-2(1H)-one derivatives 8 and 9. © 2011 American Chemical Society. Source


Kanawade S.B.,Organic Chemistry Research Center | Toche R.B.,Organic Chemistry Research Center | Patil S.P.,Organic Chemistry Research Center | Desai A.E.,K T H M College | Bhamare S.S.,K T H M College
European Journal of Medicinal Chemistry | Year: 2011

New thiophenedicarboxamide 2a-c and dicyanothiopheneacetamide 3a-c derivatives were synthesized and their bioactivity against Indoplanorbis exustus snails was evaluated. The I. exustus snail is a serious host of parasite of genus Schistosoma which infects cattle. Thus reduces livestock productivity and also acts as a source of cercarial dermatitis in human beings. The results obtained show a significant (P < 0.05) molluscicidal activity with LC 50 = 0.6043 ppm for compound 2a and LC 50 = 0.6511 ppm for compound 3a. © 2011 Elsevier Masson SAS. All rights reserved. Source

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