672325-23-4Relevant academic research and scientific papers
Efficient, chemoenzymatic process for manufacture of the boceprevir bicyclic [3.1.0]proline intermediate based on amine oxidase-catalyzed desymmetrization
Li, Tao,Liang, Jack,Ambrogelly, Alexandre,Brennan, Tim,Gloor, Guy,Huisman, Gjalt,Lalonde, James,Lekhal, Azzeddine,Mijts, Ben,Muley, Sheela,Newman, Lisa,Tobin, Matt,Wong, George,Zaks, Aleksey,Zhang, Xiyun
, p. 6467 - 6472 (2012)
The key structural feature in Boceprevir, Merck's new drug treatment for hepatitis C, is the bicyclic [3.1.0]proline moiety "P2". During the discovery and development stages, the P2 fragment was produced by a classical resolution approach. As the drug candidate advanced through clinical trials and approached regulatory approval and commercialization, Codexis and Schering-Plough (now Merck) jointly developed a chemoenzymatic asymmetric synthesis of P2 where the net reaction was an oxidative Strecker reaction. The key part of this reaction sequence is an enzymatic oxidative desymmetrization of the prochiral amine substrate.
AN IMPROVED PROCESS FOR THE PREPARATION OF RACEMIC 6, 6- DIMETHYL-3-AZABICYCLO-[3.1.0]-HEXANE AND ITS SALTS, A KEY RAW MATERIAL FOR HCV INHIBITOR.
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Page/Page column 41, (2012/05/04)
The present invention discloses an efficient and economical process for the preparation of racemic 6, 6-dimethyl-3-azabicyclo-[3.1.0]-hexane of formula I and its salts. The invention relates to the compounds of formulae I and II. The compound of formula I
PROCESS AND INTERMEDIATES FOR THE PREPARATION OF (1R,2S,5S)-6,6-DIMETHYL-3-AZABICYCLO[3,1,0]HEXANE-2-CARBOXYLATES OR SALTS THEREOF
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Page/Page column 31, (2008/06/13)
In one embodiment, the present application relates to a process of making a compound of Formula (I); and to certain intermediate compounds that are made within the process of making the compound Formula (I).
PYRAZOLOPYRIMIDINES AS CYCLIN-DEPENDENT KINASE INHIBITORS
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Page 115, (2008/06/13)
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
