1204296-03-6Relevant articles and documents
Scalable, Economical, and Practical Synthesis of 4-(Difluoromethyl)pyridin-2-amine, a Key Intermediate for Lipid Kinase Inhibitors
Rageot, Denise,Beaufils, Florent,Borsari, Chiara,Dall'asen, Alix,Neuburger, Markus,Hebeisen, Paul,Wymann, Matthias P.
, p. 2416 - 2424 (2019)
A new, scalable, rapid, high yielding, and practical synthesis of 4-(difluoromethyl)pyridin-2-amine provides a key intermediate for the preparation of numerous protein kinase inhibitors and clinical candidates targeting phosphoinositide 3-kinase (PI3K) and the mechanistic target of rapamycin (mTOR) kinase. Starting from 2,2-difluoroacetic anhydride, an efficient five-step and two-pot procedure to prepare 4-(difluoromethyl)pyridin-2-amine (1) has been developed. Noteworthy aspects of this strategy include the avoidance of an amination process using a sealed vessel. Each step of the synthetic route has been optimized, and key intermediates have been isolated and characterized prior to the final two-pot procedure, which has been successfully applied for large-scale production.
PYRROLIDINE OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 52; 53, (2016/07/05)
The present invention is directed to pyrrolidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
PYRAZOLYL PYRROLINONES AND THEIR USE AS HERBICIDES
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Page/Page column 61; 62, (2015/02/25)
The invention relates to pyrrolone compounds of the formula (I) wherein X, R1, R2, R3 and A are as defined in the specification. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising these compounds and to methods of using these compounds to control plant growth.