reductive monoalkyl- ation of amines and amine derivatives with aldehydes is reported. Treatment of aldehydes with primary amines, secondaryamines, O- trimethylsilylhydroxylamine, and N,N-dimethylhydrazine in lithi- um perchlorate/diethylether and trimethylsilyl chloride, followed by BH3·NEt3 reduction, and straightforward workup afforded sec- ondary amines, tertiary amines, N-substituted hydroxylamines
[EN] NECROSIS INHIBITORS<br/>[FR] INHIBITEURS DE NÉCROSE
申请人:NAT INST OF BIOLOG SCIENCES BEIJING
公开号:WO2016101885A1
公开(公告)日:2016-06-30
The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
[EN] PYRIMIDINE DERIVATIVES AND THEIR USE AS CB2 MODULATORS<br/>[FR] DERIVES DE PYRIMIDINE ET LEUR UTILISATION EN TANT QUE MODULATEURS CB2
申请人:GLAXO GROUP LTD
公开号:WO2004018433A1
公开(公告)日:2004-03-04
This relates to novel pyrimidine derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrease in activity of the cannabinoid receptor.
A [3 + 3] formal cycloaddition reactionbetween in situ formed azaoxyallyl cations and nitrones from isatins has been developed, furnishing a spectrum of spiro[1,2,4‐oxadiazinan‐5‐one]oxindoles in good to excellent yields with excellent diastereoselectivity. This method provides direct and efficient access to potentially bioactive spirooxindoles incorporating a six‐membered heterocyclic scaffold.
bromides and chlorides with aqueous ammonia and hydroxylamine was achieved in continuous flow to produce primary ammonium salts and hydroxylamines in high yields. An in-line workup was designed to isolate the corresponding primary amine, which was also telescoped in further reactions, such as acylation and Paal–Knorr pyrrole synthesis. Monosubstituted epoxides are also compatible with the reaction conditions