Saturated aza-heterocycles are highly privileged building blocks that are commonly
encountered in bioactive compounds and approved therapeutic agents. These N …

As a naturally occurring small‐molecule, various optical isomers of chiral pyrrolo [2, 1‐a]
isoquinoline alkaloid crispine A represent a potential class of chiral molecules in …

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Enantioenriched 2-aryl azepanes and 2-arylbenzazepines were generated biocatalytically
by asymmetric reductive amination using imine reductases or by deracemization using …

Aryl and heteroaryl rings are omnipresent in small molecule drugs, and examples bearing
multiple substitutions at benzylic positions are ubiquitous across a range of pharmaceutical …

A new method for the synthesis of enantiopure α-substituted piperazines via direct
functionalization of the intact piperazine ring is described. The approach utilizes the …

The palladium‐catalyzed ligand‐controlled arylation of α‐zincated acyclic amines, obtained
by directed α‐lithiation and transmetalation, is described. Whereas PtBu3 gave rise to α …

Lithiation of N-Boc-1-phenyltetrahydroisoquinolines was optimized by in situ IR
spectroscopy. The kinetics for rotation of the carbamate group and for the enantiomerization …

α-Amino nitrile 2a was conveniently prepared in two individual steps from chiral
hexafluorophosphate salt isoquinolinium (−)-8b including anodic cyanation as an efficient …

Treatment of N-Boc-2-aryl-1, 2, 3, 4-tetrahydroquinolines with n-butyllithium in THF at− 78° C
resulted in efficient lithiation at the 2-position and the organolithiums were trapped with a …