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Perfluoroalkylated indoles are valuable compounds in drug discovery. A Pd(0)-catalyzed C(sp(3))-H functionalization enables access to 2-(trifluoromethyl)indoles from trifluoroacetimidoyl chlorides. These are stable compounds, easily obtained from anilines. ...
Cyclopropanes fused to pyrrolidines are important structural features found in a number of marketed drugs and development candidates. Typically, their synthesis involves the cyclopropanation of a dihydropyrrole precursor. Reported herein is a complementary ...
Taddol-based phosphoramidite ligands enable enantioselective palladium(0)-catalyzed C-H arylation of cyclopropanes. The cyclized products are obtained in high yields and enantioselectivities. The reported method provides efficient access to a broad range o ...
An enantioselective C-H arylation of phosphine oxides with o-quinone diazides catalyzed by an iridium(III) complex bearing an atropchiral cyclopentadienyl (Cp-x) ligand and phthaloyl tert-leucine as co-catalyst is reported. The method allows access to a) P ...
Transition-metal catalysed enantioselective CâH functionalisations enable rapid increase of molecular complexity via non-classical disconnections. This thesis describes the development of intramolecular Pd(0)-catalysed C-H functionalisations for the asym ...
beta-Lactams are very important structural motifs because of their broad biological activities as well as their propensity to engage in ring-opening reactions. Transitionmetal- catalyzed C-H functionalizations have emerged as strategy enabling yet uncommon ...
Monodentate TADDOL-derived phosphoramidites and phosphonites are versatile chiral ligands for enantio-selective Pd(0)-catalysed C-H functionalisations. They enable highly selective cyclisations to access a wide range of chiral carbo-and heterocycles. The h ...
An enantioselective C-H functioffalization route to perfluoroalkyl-containing 3-azabicyclo[3.1.0]-hexanes is disclosed. A modular and bench-stable diazaphospholane ligand enables highly enantioselective Pd(0)-catalyzed cyclopropane C-H functionalization us ...