Sulfoximines from a medicinal chemist's perspective: physicochemical and in vitro parameters relevant for drug discovery
M Frings, C Bolm, A Blum, C Gnamm - European Journal of Medicinal …, 2017 - Elsevier
Sulfoximines, sulfondiimides and sulfonimidamides are fascinating but not yet fully explored
variants of the common sulfone or sulfonamide motif. In this study, we report the …
variants of the common sulfone or sulfonamide motif. In this study, we report the …
Straightforward strategies for the preparation of NH-sulfoximines: a serendipitous story
Sulfoximines are emerging as valuable new isosteres for use in medicinal chemistry, with
the potential to modulate physicochemical properties. Recent developments in synthetic …
the potential to modulate physicochemical properties. Recent developments in synthetic …
Dioxazolones: stable substrates for the catalytic transfer of acyl nitrenes
KM van Vliet, B de Bruin - ACS Catalysis, 2020 - ACS Publications
Dioxazolones are a convenient class of acyl nitrene transfer reagents. Their application in
homogeneous transition-metal catalysis has led to many new amidation reactions …
homogeneous transition-metal catalysis has led to many new amidation reactions …
Transfer of electrophilic NH using convenient sources of ammonia: direct synthesis of NH sulfoximines from sulfoxides
A new system for NH transfer is developed for the preparation of sulfoximines, which are
emerging as valuable motifs for drug discovery. The protocol employs readily available …
emerging as valuable motifs for drug discovery. The protocol employs readily available …
Cationic Cobalt (III)‐Catalyzed Aryl and Alkenyl C H Amidation: A Mild Protocol for the Modification of Purine Derivatives
A cationic cobalt (III)‐catalyzed direct C H amidation of unactivated (hetero) arenes and
alkenes by using 1, 4, 2‐dioxazol‐5‐ones as the amidating reagent has been developed …
alkenes by using 1, 4, 2‐dioxazol‐5‐ones as the amidating reagent has been developed …
Mechanochemical rhodium (III)-catalyzed C–H bond amidation of arenes with dioxazolones under solventless conditions in a ball mill
GN Hermann, C Bolm - ACS Catalysis, 2017 - ACS Publications
A procedure for the direct mechanochemical rhodium (III)-catalyzed C–H bond amidation of
arenes with 1, 4, 2-dioxazol-5-ones as the nitrogen source has been developed. The …
arenes with 1, 4, 2-dioxazol-5-ones as the nitrogen source has been developed. The …
Study of sustainability and scalability in the Cp* Rh (III)-catalyzed direct C–H amidation with 1, 4, 2-dioxazol-5-ones
The practical aspects of Cp* Rh (III)-catalyzed direct C–H amidation with 1, 4, 2-dioxazol-5-
ones were investigated on the operational safety, use of green solvent, and scalability …
ones were investigated on the operational safety, use of green solvent, and scalability …
Mechanistic investigation of the NH-sulfoximination of sulfide. Evidence for λ 6-sulfanenitrile intermediates
JF Lohier, T Glachet, H Marzag, AC Gaumont… - Chemical …, 2017 - pubs.rsc.org
We report a new procedure for the preparation of NH-sulfoximines from sulfides using PIDA
as an oxidant and ammonium carbamate as the ammonia source. Excellent yields were …
as an oxidant and ammonium carbamate as the ammonia source. Excellent yields were …
Mechanochemical Cobalt‐Catalyzed C− H Bond Functionalizations by Ball Milling
Ball milling techniques have been applied in the development of a mechanosynthesis of
[Cp* Co (CO) I2], which proved highly efficient as catalyst in mechanochemical C− H bond …
[Cp* Co (CO) I2], which proved highly efficient as catalyst in mechanochemical C− H bond …
Synthesis of sulfoximine carbamates by rhodium-catalyzed nitrene transfer of carbamates to sulfoxides
Sulfoximines are of considerable interest for incorporation into medicinal compounds. A
convenient synthesis of N-protected sulfoximines is achieved, under mild conditions, by …
convenient synthesis of N-protected sulfoximines is achieved, under mild conditions, by …