Jubilee Hills, India
Jubilee Hills, India

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Raju V.,Srini Pharmaceuticals Ltd | Somaiah S.,Srini Pharmaceuticals Ltd | Sashikanth S.,Srini Pharmaceuticals Ltd | Laxminarayan E.,Mahatma Gandhi Institute | Mukkanti K.,Jawaharlal Nehru University
Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry | Year: 2014

An asymmetric synthesis of (S)-levetiracetam has been developed through application of a Strecker reaction using [(1S)- 1-(4-methoxyphenyl)ethyl]amine hydrochloride as a chiral auxiliary. Addition of propanaldehyde to a solution of sodium cyanide and [(1S)-1-(4-methoxyphenyl)ethyl]amine hydrochloride in the mixture of methanol and water at 25-30°C afforded diastereomerically pure 2-[2-(4-methoxyphenyl)-(S)-methylethyl-amino]-( S )-butyronitrile hydrochloride compound 4 . In this reaction cyanide group attack at less hindered side that is re-face of the imine intermediate gave the diastereomerically pure nitrile 4. Which upon hydrolysis in the presence of 6 M aqueous hydrochloride solution obtained enantiomerically pure (S )-2- aminobutyric acid hydrochloride 5, is a key intermediate for the (S)-levetiracetam. This intermediate further react with SOCl2 in presence of methanol formed S-2-amino methyl butyrate as in situ intermediate which on further ammonalysis in the presence of methnaolic ammonia as a solvent under ammonia pressure provided S-2-amino butyramide hydrochloride 6 which further condensed with 4-chlorobutyryl chloride 7 and followed by cyclization in the presence of potassium hydroxide, dichloromethane solvent used catalytic amount of tetra butyl ammonium bromide afforded crude (S)-levetiracetam 1, further recrystalization in the presence of ethyl acetate obtained pure (S)-levetiracetam 1. © 2014, Scientific Publishers. All rights reserved.


Rao S.N.,Srini Pharmaceuticals Ltd. | Ravisankar T.,Srini Pharmaceuticals Ltd. | Latha J.,Krishna University | Sudhakar Babu K.,Krishna University
Der Pharma Chemica | Year: 2012

A series of novel biphenyl tetrazoles compounds have been prepared from the secondary amides by the reaction with phosphorous pentachloride and sodium azide. These tetrazoles compounds were subjected to benzylic bromination and further condensed with n-methyl piperazine to afford compounds 6a-j and 7. The structures of the newly synthesized compounds were characterized by NMR, Mass, IR spectral data and elemental analysis. All the synthesized compounds were screened for their antibacterial activity.


Rao S.N.,Srini Pharmaceuticals Ltd. | Babu K.S.,Krishna University
Organic Communications | Year: 2011

Development of a new improved and efficient process suitable for the large-scale production of Irbesartan has been described. The key steps are tetrazole formation from secondary amide for the preparation of the key intermediate 1-Benzyl-5-(4'-bromomethyl-biphenyl-2-yl)-1H-tetrazole (9), N-alkylation and debenzylation. © 2011 Reproduction is free for scientific studies.


Rao S.N.,Srini Pharmaceuticals Ltd. | Sitaramaiah D.,Srini Pharmaceuticals Ltd. | Srimannarayana K.,Srini Pharmaceuticals Ltd. | Rao C.N.,Srini Pharmaceuticals Ltd. | And 3 more authors.
Synthetic Communications | Year: 2011

Carvedilol (Coreg) is a nonselective -adrenergic blocking agent with vasodilating activity. It is used for the treatment of congestive heart failure and hypertension. During the bulk synthesis of carvedilol, we have observed six impurities: Imp-I, Imp-II, Imp-III, Imp-IV, Imp-V, and Imp-VI. The present work describes the synthesis and characterization of these impurities. Copyright © 2011 Taylor and Francis Group, LLC.


Muralidhar A.,Sri Krishnadevaraya University | Babu K.S.,Sri Krishnadevaraya University | sankar T.R.,Srini Pharmaceuticals Ltd | Reddanna P.,University of Hyderabad | Latha J.,Sri Krishnadevaraya University
International Journal of Phytomedicine | Year: 2011

The study aims to evaluate the wound healing properties of bioactive fractions from the extract of Butea monosperma (Lam) stem bark. In this study the stem bark powder was extracted with ethanol, further the ethanolic extract was fractionated with different solvents (petroleum ether, benzene, chloroform and acetone) in increasing order of polarity. Thus prepared extracts were subjected to preliminary phytochemical analysis. The wound healing activity of the ethanolic extract and the fractions isolated from the stem bark of Butea monosperma were evaluated in excision, incision and dead space wound healing models using Albino wistar rats. The wound healing activity was assessed by the breaking strength in case of incision wounds, epithelialization and wound contraction in case of excision wound and granulation tissue dry weight, breaking strength and hydroxyproline content in case of dead space wound. The ethanolic extract and the acetone fraction showed the significant wound healing activity on all three wound models. The phytochemical investigations revealed the presence of alkaloids, tannins, flavonoids, phenolic compounds and steroids. The increased rate of wound contraction and hydroxyproline content in the ethanolic extract and the acetone fraction treated animals provides a scientific base to the ethno medicinal use of Butea monosperma, which is largely attributable to the additive or synergistic effect of their constituents.


Somaiah S.,Srini Pharmaceuticals Ltd. | Sashikanth S.,Srini Pharmaceuticals Ltd. | Raju V.,Srini Pharmaceuticals Ltd. | Reddy K.V.,Osmania University
Tetrahedron Asymmetry | Year: 2011

An asymmetric conjugate addition reaction between a chiral α,β-unsaturated amido ester and ethyl-N-methylmalonamide has been used as a key step in the synthesis of (3S,4R)-(-)-trans-4-(4′- fluorophenyl)-3-hydroxymethyl-N-methylpiperidine, a key intermediate for (-)-paroxetine. © 2011 Elsevier Ltd. All rights reserved.


Challa N.R.,Srini Pharmaceuticals Ltd. | Challa N.R.,Osmania University | Mamidisetty B.,Srini Pharmaceuticals Ltd. | Ghanta M.R.,Macleods Pharmaceuticals Ltd. andheri East | Padi P.R.,Macleods Pharmaceuticals Ltd. andheri East
Journal of Saudi Chemical Society | Year: 2014

One pot synthesis and characterization of new 5-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-4,5,6,7-tetrahydro-thieno[3,2-c]pyridines (. 3a-k) using amides (. 2a-k) were reported. The prepared 5-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-4,5,6,7-tetrahydro-thieno[3,2-c]pyridine (. 3a) is a bioisostere of 4'-(6,7-dihydro-4H-thieno [3,2-c]pyridin-5-ylmethyl)-biphenyl-2-carboxylic acid (. 1), having good in vivo antithrombotic activity compared with Clopidogrel. The new tetrazole derivatives (. 3a-k) were screened for their in vitro activity as platelet aggregation inhibitors. © 2011 .


Sashikanth S.,Srini Pharmaceuticals Ltd | Raju V.,Srini Pharmaceuticals Ltd | Somaiah S.,Srini Pharmaceuticals Ltd | Rao P.,Srini Pharmaceuticals Ltd | Reddy K.,Osmania University
Synthesis (Germany) | Year: 2013

An asymmetric synthesis of (S)-(+)-clopidogrel hydrogen sulfate has been developed through application of a Strecker reaction with [(1S)-1-(4- methoxyphenyl)ethyl]amine hydrochloride as a chiral auxiliary. Addition of 2-chlorobenzaldehyde to a solution of sodium cyanide and [(1S)-1-(4- methoxyphenyl)ethyl]amine hydrochloride gave diastereoisomerically pure (2S)-(2-chlorophenyl){[(1S)-1-(4-methoxyphenyl)ethyl]amino}acetonitrile hydro chloride. Cleavage of the chiral auxiliary and concomitant hydrolysis of the nitrile group then gave enantiomerically pure (2S)-2-(2-chlorophenyl)glycine hydrochloride, a key intermediate for (S)-(+)-clopidogrel. © Georg Thieme Verlag Stuttgart. New York.


Rao C.N.,Srini Pharmaceuticals Ltd. | Naresh T.,Srini Pharmaceuticals Ltd. | Satyanarayana K.,Srini Pharmaceuticals Ltd. | Reddy B.R.,Srini Pharmaceuticals Ltd. | Reddy G.M.,Inogent Laboratories Private Ltd.
Synthetic Communications | Year: 2010

Cost-effective and improved one-pot synthesis for telmisartan (1) is described that minimizes the reaction time and gives high-purity material. Copyright © Taylor & Francis Group, LLC.


Challa N.R.,Srini Pharmaceuticals Ltd | Challa N.R.,Osmania University | Ghantac M.R.,Macleods Pharmaceuticals Ltd andheri East Mumbai | Padic P.R.,Macleods Pharmaceuticals Ltd andheri East Mumbai
Letters in Organic Chemistry | Year: 2011

During the course of our investigation in the field of thienopyridine based antithrombotic agents, we have identified and synthesized 4'-(6,7-dihydro-4H- thieno[3,2-c]pyridin-5-ylmethyl)-biphenyl-2-carboxylic acid derivatives 5a-i, a thienopyridine derivative with good in vivo activity against thrombus formation. These findings prompted us to prepare new 4'-(6,7-dihydro-4H-thieno[3,2-c] pyridin-5-ylmethyl)-bipheny1-2-carboxylic acid derivatives bearing different acid derivatives 5a-i in the hope of increasing activity and better understanding the influence of esters and amides on the thrombus formation. © 2011 Bentham Science Publishers Ltd.

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