Abstract: The present invention provides an improved process for preparation of (E)-?-[[2-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1H-imidazole-5-yl]methylene]-2-thiophene propanoic acid ethyl ester in high purity and in high yield. Thus, for example, 4-[[2-butyl-5-formyl-1H-imidazole-1-yl]methyl]benzoic acid methyl ester is reacted with ethyl 2-carboxy-3-(2-thienyl)propionate in the presence of piperidinium propionate in diisopropyl ether or a mixture of n-hexane and a solvent selected from toluene and cyclohexane, optionally purifying the crude compound to obtain (E)-?-[[2-butyl-1-[[4-(methoxy carbonyl)phenyl]methyl]-1H-imidazole-5-yl]methylene]-2-thiophene propanoic acid ethyl ester substantially free of 3-(2-thienyl)propanoic acid ethyl ester impurity.
Type:
Application
Filed:
March 31, 2008
Publication date:
March 3, 2011
Applicant:
HETERO RESEARCH FOUNDATION
Inventors:
Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muraldihara Reddy, Medabalimi Peter Paul Raj
Abstract: The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
Type:
Application
Filed:
July 2, 2010
Publication date:
January 20, 2011
Applicant:
HETERO RESEARCH FOUNDATION
Inventors:
Bandi PARTHASARADHI REDDY, Vedula MANOHAR SHARMA, Kura RATHNAKAR REDDY, Musku MADHANMOHAN REDDY, Nelli YELLA REDDY, Lanka VL SUBRAHMANYAM
Abstract: There was provided a process for preparing candesartan cilexetil, the said process comprises hydrogenating a solution of trityl candesartan cilexetil in an alcohol with hydrogen in the presence of a palladium catalyst. Mixture of toluene and methanol was added to 1-(Cyclohexyloxy carbonyloxy)ethyl-2-ethoxy-1-[[2?-(N-triphenylmethyltetrazole-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and hydrogenated at room temperature with hydrogen at atmospheric pressure in the presence of palladium on carbon until the hydrogen uptake was ceased. Filtered over celite bed, washed the bed with a mixture of toluene and methanol, filtrate was collected and concentrated. Co-distilled with acetonitrile, acetonitrile was added, stirred at room temperature, cooled to 0° C. stirred, filtered, washed with chilled acetonitrile and dried to get candesartan cilexetil.