Synthesis of Polyfunctional Secondary Amines by the Reaction of Functionalized Organomagnesium Reagents with Tertiary Nitroalkanes
作者:Paul Knochel、Vasudevan Dhayalan
DOI:10.1055/s-0034-1378871
日期:——
Abstract Addition of polyfunctionalized aryl, heteroaryl, and tertiary alkylmagnesium reagents to tertiary nitroalkanes at 25 °C in tetrahydrofuran produces, after reductive workup with FeCl2 and NaBH4 in ethanol, the corresponding polyfunctional secondaryamines in high yields. Addition of polyfunctionalized aryl, heteroaryl, and tertiary alkylmagnesium reagents to tertiary nitroalkanes at 25 °C in
Amination of diaryl sulfoxides with anilines and alkylamines has been accomplished under palladium/N-heterocyclic carbene (NHC) catalysis. Owing to its electron deficiency, the leaving arenesulfenate anion would be smoothly released from the palladium center to result in uneventful catalyst turnover under milder reaction conditions in comparison with previous C–S bond amination reactions. This amination
The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:
which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
The present invention provides compounds of formula I
and pharmaceutically acceptable salts thereof.
The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.