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Patent
Jubilant Life science Ltd | Date: 2012-10-19

The present invention provides a novel process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, or a salt thereof, preferably Aliskiren hemifumarate.


Patent
JUBILANT LIFE science LTD | Date: 2011-09-12

Disclosed herein cost effective and ecofriendly large scale process for producing pyridine carboxylic acid with high purity and yield at industrial scale.


The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-()-10-hydroxy-dihydrodibenz[b,f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The present invention also provides use of thus prepared (S)-(+)- or (R)-()-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-()-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J


The invention relates to a substantially pure linezolid hydroxide having R-isomer content more than about 99.9% relative to its S-isomer. Further aspect of invention provides the ambient moisture condition, which is critical for enantiomeric pure linezolid hydroxide. The obtained substantially enantiomerically pure linezolid hydroxide compound of formula-II can be subsequently converted into the linezolid compound of formula-I, having S-isomer content more than 99.9% relative to R-isomer. Further the invention provides an improved process for preparation of enantiomeric pure linezolid Form-I, wherein linezolid Form-I having the purity more than 99.9% relative to any other known polymorphic form of linezolid. The obtained enantiomeric pure linezolid Form-I can be subsequently converted into the other known polymorphic forms linezolid. The invention also provides stable and substantially solvent-free crystal of Form-I of linezolid.


Thomas S.,Jubilant Life science Ltd. | Mathela C.S.,Kumaun University | Agarwal A.,Jubilant Life science Ltd. | Paul S.K.,Jubilant Life science Ltd.
Journal of Pharmaceutical and Biomedical Analysis | Year: 2011

Two impurities were detected in the HPLC analysis of crude carbamazepine active pharmaceutical ingredient. One of the impurities of the order of 0.5% was found to be unknown and has not been reported previously. A LC-MS compatible reverse phase isocratic method was developed and tandem mass spectrometry was performed using electrospray ionization source and ion trap mass analyzer. Isolation of unknown impurity was performed by semi-preparative HPLC followed by characterization using nuclear magnetic resonance spectroscopy (NMR), infrared spectroscopy (FT-IR) and elemental analysis (CHNS) confirmed its structure as tetrabenzo[b,f,b′f′]azepino[4′,5′:4,5]thieno[2,3- d]azepine-3,9-dicarboxamide. A plausible mechanism for the formation of this impurity is proposed. © 2011 Elsevier B.V. Source

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