Adam P. Smalley
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View article: Modular, Automated Synthesis of Spirocyclic Tetrahydronaphthyridines from Primary Alkylamines
Modular, Automated Synthesis of Spirocyclic Tetrahydronaphthyridines from Primary Alkylamines Open
Spirocyclic tetrahydronaphthyridines (THNs) are valuable scaffolds for drug discovery campaigns, but access to this 3D chemical space is hampered by a lack of modular and scalable synthetic methods. We hereby report a fully automated, cont…
View article: CCDC 2074252: Experimental Crystal Structure Determination
CCDC 2074252: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Palladium-Catalyzed Enantioselective C–H Activation of Aliphatic Amines Using Chiral Anionic BINOL-Phosphoric Acid Ligands
Palladium-Catalyzed Enantioselective C–H Activation of Aliphatic Amines Using Chiral Anionic BINOL-Phosphoric Acid Ligands Open
The design of an enantioselective Pd(II)-catalyzed C-H amination reaction is described. The use of a chiral BINOL phosphoric acid ligand enables the conversion of readily available amines into synthetically valuable aziridines in high enan…
View article: CCDC 1522637: Experimental Crystal Structure Determination
CCDC 1522637: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: A general catalytic β-C–H carbonylation of aliphatic amines to β-lactams
A general catalytic β-C–H carbonylation of aliphatic amines to β-lactams Open
CO takes the lead to make β-lactam rings Strained β-lactam rings are a key feature of penicillin and some other drugs. Willcox et al. designed a versatile route to these four-membered ring motifs through the palladiumcatalyzed coupling of …
View article: Continuous‐Flow Synthesis and Derivatization of Aziridines through Palladium‐Catalyzed C(sp<sup>3</sup>)−H Activation
Continuous‐Flow Synthesis and Derivatization of Aziridines through Palladium‐Catalyzed C(sp<sup>3</sup>)−H Activation Open
A continuous‐flow synthesis of aziridines by palladium‐catalyzed C(sp 3 )−H activation is described. The new flow reaction could be combined with an aziridine‐ring‐opening reaction to give highly functionalized aliphatic amines through a c…
View article: Continuous‐Flow Synthesis and Derivatization of Aziridines through Palladium‐Catalyzed C(sp<sup>3</sup>)−H Activation
Continuous‐Flow Synthesis and Derivatization of Aziridines through Palladium‐Catalyzed C(sp<sup>3</sup>)−H Activation Open
A continuous‐flow synthesis of aziridines by palladium‐catalyzed C(sp 3 )−H activation is described. The new flow reaction could be combined with an aziridine‐ring‐opening reaction to give highly functionalized aliphatic amines through a c…