142148-11-6Relevant academic research and scientific papers
SUBSTITUTED PYRAZOLOAZEPIN-4-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 112; 113, (2018/07/05)
The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
PYRIDYL OR PYRAZINYL COMPOUNDS CARRYING A METHYL-BOUND ALPHA-AMINO ACID AMIDE GROUP
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Page/Page column 197, (2017/04/11)
The present invention relates to pyridyl or pyrazinyl compounds carrying a methyl- bound N-amide moiety derived from an α-amino acid of formula I where the variables are as defined in the claims and the description. The invention further relates to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, and to their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of the 5-HT2C receptor.
Selective mono-acylation of 1,2- and 1,3-diols using (α,α- difluoroalkyl)amines
Wakita, Natsumi,Hara, Shoji
experimental part, p. 7939 - 7945 (2010/10/19)
In the reaction of N,N-diethyl-α,α-difluorobenzylamine (DFBA) with 1,2- or 1,3-diols, selective mono-benzoylation occurs to afford mono-esters of the diols in good yield. The reaction is completed under mild conditions in a short reaction time. Further, prim-, sec-, and tert-diols and catechol can be converted to the corresponding mono-benzoates. DFBA is used for the protection of the hydroxy group in sugars. The selective mono-nicotinylation, formylation and pivaloylation of diols are also performed by using the corresponding difluoroalkylamines.
