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 …

Straightforward strategies for the preparation of NH-sulfoximines: a serendipitous story

JA Bull, L Degennaro, R Luisi - Synlett, 2017 - thieme-connect.com
Sulfoximines are emerging as valuable new isosteres for use in medicinal chemistry, with
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 …

Transfer of electrophilic NH using convenient sources of ammonia: direct synthesis of NH sulfoximines from sulfoxides

M Zenzola, R Doran, L Degennaro, R Luisi… - Angewandte …, 2016 - Wiley Online Library
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 …

Cationic Cobalt (III)‐Catalyzed Aryl and Alkenyl C H Amidation: A Mild Protocol for the Modification of Purine Derivatives

Y Liang, YF Liang, C Tang, Y Yuan… - Chemistry–A European …, 2015 - Wiley Online Library
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 …

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 …

Study of sustainability and scalability in the Cp* Rh (III)-catalyzed direct C–H amidation with 1, 4, 2-dioxazol-5-ones

Y Park, S Jee, JG Kim, S Chang - Organic Process Research & …, 2015 - ACS Publications
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 …

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 …

Mechanochemical Cobalt‐Catalyzed C− H Bond Functionalizations by Ball Milling

H Cheng, JG Hernández, C Bolm - Advanced Synthesis & …, 2018 - Wiley Online Library
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 …

Synthesis of sulfoximine carbamates by rhodium-catalyzed nitrene transfer of carbamates to sulfoxides

M Zenzola, R Doran, R Luisi, JA Bull - The Journal of Organic …, 2015 - ACS Publications
Sulfoximines are of considerable interest for incorporation into medicinal compounds. A
convenient synthesis of N-protected sulfoximines is achieved, under mild conditions, by …