4 research outputs found
Ir-Catalyzed Preparation of SF<sub>5</sub>鈥慡ubstituted Potassium Aryl Trifluoroborates via C鈥揌 Borylation and Their Application in the Suzuki鈥揗iyaura Reaction
The preparation of new pentafluorosulfanyl-substituted potassium aryltrifluoroborates via Ir-catalyzed C鈥揌 borylation is reported. The utility of these novel building blocks was demonstrated in the Suzuki鈥揗iyaura cross-coupling reaction, giving access to 3,5-disubstituted pentafluorosulfanylbenzenes
Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries
The synthesis and diversification of a densely functionalized
azetidine
ring system to gain access to a wide variety of fused, bridged, and
spirocyclic ring systems is described. The in vitro physicochemical
and pharmacokinetic properties of representative library members are
measured in order to evaluate the use of these scaffolds for the generation
of lead-like molecules to be used in targeting the central nervous
system. The solid-phase synthesis of a 1976-membered library of spirocyclic
azetidines is also described
Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries
The synthesis and diversification of a densely functionalized
azetidine
ring system to gain access to a wide variety of fused, bridged, and
spirocyclic ring systems is described. The in vitro physicochemical
and pharmacokinetic properties of representative library members are
measured in order to evaluate the use of these scaffolds for the generation
of lead-like molecules to be used in targeting the central nervous
system. The solid-phase synthesis of a 1976-membered library of spirocyclic
azetidines is also described
Synthesis and Profiling of a Diverse Collection of Azetidine-Based Scaffolds for the Development of CNS-Focused Lead-like Libraries
The synthesis and diversification of a densely functionalized
azetidine
ring system to gain access to a wide variety of fused, bridged, and
spirocyclic ring systems is described. The in vitro physicochemical
and pharmacokinetic properties of representative library members are
measured in order to evaluate the use of these scaffolds for the generation
of lead-like molecules to be used in targeting the central nervous
system. The solid-phase synthesis of a 1976-membered library of spirocyclic
azetidines is also described