- Synthesis and Process Optimization of Boceprevir: A Protease Inhibitor Drug
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Efforts toward the synthesis and process optimization of boceprevir 1 are described. Boceprevir synthesis was optimized by telescoping the first three steps and last two steps of the five-step process. Optimization of oxidation, which is one of the critical steps in the total synthesis, is discussed. A control strategy for the three impurities is described. A novel process for the synthesis of fragment A (2) has been developed, which is the key starting material for the synthesis of boceprevir.
- Bhalerao, Dinesh S.,Arkala, Anil Kumar Reddy,Madhavi,Nagaraju,Gade, Srinivas Reddy,Kumar, U. K. Syam,Bandichhor, Rakeshwar,Dahanukar, Vilas H.
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p. 1559 - 1567
(2015/11/28)
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- PROCESS FOR PREPARATION OF BOCEPREVIR AND INTERMEDIATES THEREOF
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THE PRESENT INVENTION RELATES TO AN IMPROVED PROCESS FOR THE PREPARATION OF (1R,5S)-N-[3-AMINO-1-(CYCLOBUTYLMETHYL)-2,3-DIOXOPROPYL]-3-[2(S)-[[[(1,1-DIMETHYLETHYL)AMINO]CARBONYL] AMINO]-3,3-DIMETHYL-1-OXOBUTYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2(S)-CARBOXAMIDE AND ITS INTERMEDIATES
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Page/Page column 33; 38
(2014/05/07)
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- PROCESS FOR PRODUCTION OF N-CARBAMOYL-TERT-LEUCINE
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The present invention relates to a process for producing an N-carbamoyl-tert-leucine, characterized in mixing tert-leucine with an isocyanic acid compound while a pH of the mixture is kept at not less than 8.0 and not more than 13.5, wherein an amount of the isocyanic acid compound is not less than 0.9 times by mole and not more than 1.1 times by mole relative to an amount of the tert-leucine. According to the present invention, it becomes possible to easily produce an N-carbamoyl-tert-leucine with high efficiency, while the generation of by-products such as a dipeptide-like compound and a urea compound is prevented.
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Page/Page column 6-7
(2010/09/05)
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- PROCESS FOR THE PREPARATION OF (S)-2-(3-TERT-BUTYLUREIDO)-3,3-DIMETHYLBUTANOIC ACID
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(S)-2-(3-tert-Butylureido)-3,3-dimethylbutanoic acid is conveniently prepared in a single reaction vessel from commercially available starting materials in a process that can be run on a kilogram or larger scale.
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Page/Page column 7-8
(2009/04/25)
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- HEPATITIS C VIRUS INHIBITORS
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Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of formula (I): wherein B, X, R3, L0, L1, L2, R2, R1 and RC are defined herein. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
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