SARS-COV-2 INHIBITORS HAVING COVALENT MODIFICATIONS FOR TREATING CORONAVIRUS INFECTIONS
Provided herein are compounds, pharmaceutical compositions and methods for treating a SARS-CoV-2 infection.
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(2021/11/06)
One-Pot Generation of Benzynes from Phenols: Formation of Primary Anilines by the Deoxyamination of Phenols
Benzynes were selectively generated in situ from phenols and trapped regioselectively with potassium hexamethyldisilazide to form primary anilines following acidic workup. The direct conversion of a phenolic hydroxyl group into a free amino group is a useful method for the preparation of primary aryl amines that are hard to synthesize by using coupling reactions involving phenol derivatives with ammonia. Whereas reactions of ortho- and meta-substituted phenols produced meta-substituted anilines exclusively, those of para-substituted phenols provided ortho-silylanilines.
Akai, Shuji,Ikawa, Takashi,Masuda, Shigeaki
(2020/03/23)
SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS
The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).
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Page/Page column 99
(2010/02/13)
1,3-Disubstituted benzazepines as novel, potent, selective neuropeptide Y Y1 receptor antagonists
A novel series of potent and selective non-peptide neuropeptide Y (NPY) Y1 receptor antagonists, having benzazepine nuclei, have been designed, synthesized, and evaluated for activity. Chemical modification of the R1 and R3 substitue