Absolute configuration of boceprevir chiral fragment-B by chiral chromatographic, spectroscopic, thermal and crystallization techniques

Boceprevir is a protease inhibitor ,it cures the hepatitis caused by hepatitis C virus genotype 1,it binds to the HCV nonstructural protein 3 active site[1],The chiral fragment of Boceprevir drug substance is plays key role for the activity on chronic hepatitis C infection[2]. Development and valida...

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Bibliographic Details
Published in:Asian Journal of Research in Chemistry 2018-05, Vol.11 (3), p.671-680
Main Authors: Rajana, Nagaraju, Pallavi, V., Madhavan, P., Mohan, H. Rama, Babu, J. Moses, Basavaiah, K.
Format: Article
Language:English
Subjects:
Chromatography
Configurations
Conflicts of interest
Crystallization
Crystallography
Cures
Drug dosages
Ethanol
Evaporation
Hepatitis
Hepatitis C
Infrared analysis
Laboratories
NMR
Nuclear magnetic resonance
Pharmaceuticals
Potassium
Proteinase inhibitors
Single crystals
Software
Thermal analysis
Viruses
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Summary:Boceprevir is a protease inhibitor ,it cures the hepatitis caused by hepatitis C virus genotype 1,it binds to the HCV nonstructural protein 3 active site[1],The chiral fragment of Boceprevir drug substance is plays key role for the activity on chronic hepatitis C infection[2]. Development and validation of stability-indicating hptlc method for determination of boceprevir[8].As per the author knowledge no method was explained the absolute configuration of Chiral fragment of Boceprevir, but in this work the author as proposed that the absolute configuration of Chiral fragment of Boceprevi-B, this was confirmed Normal phase chromatography, ID NMR, SOR, FT-IR ,Thermal analysis PXRD and single crystal. Synthesis of Boceprevir Fragment-B single crystal. methyl(1R,2S,5S)-6,6-dimethyl-3-azabicyclo[3.1.0] hexane-2-carboxylate hydrochloride was synthesized by slow evaporation technique, in this procedure the pure 15 mg Boceprevir Fragment-b was taken in 25 mL volumetric flask containing 7.5 mL of Dichloro methane and added 7.5 mL of di isopropyl ether and properly mixed by vortex mixer and covered with parafilm and made it holes for slow evaporation after 2-6 hrs, needle shaped crystal were obsereved by microscopic image Figure.3.
ISSN:0974-4169
0974-4150
DOI:10.5958/0974-4150.2018.00120.7