A mild and practical protocol for the copper-mediated trifluoromethylation of aryl and heteroaryl boronic acids using NaSO2CF3 (Langlois' reagent) and TBHP is described. The reaction proceeds at room temperature under am...
Hoveyda-Grubbs' catalyst is able to catalyze crossed [2 + 2 + 2] cyclotrimerizations of diynes with nitriles. Pyridines are obtained with excellent yields when using activated nitriles and low to moderate yields with non...
Five rigid oxadiazole (OXD) containing silanes, denoted 1-5, have been developed with high morphological stability. Disruption of the pi-aromatic conjugation by introduction of Si atoms leads to a large band gap and high...
The first enantioselective copper-catalyzed cyclopropanation of N-acyl indoles is described. Using carbohydrate-based bis(oxazoline) ligands (glucoBox), the products were obtained in up to 72% ee. Cyclopropanation of N-B...
Unprecedented aryne Diels-Alder reactions by using methyleneindolinones as dienes have been disclosed, thus providing a quick access to unusual naphtho-fused oxindoles. A wide range of methyleneindolinones proceed readil...
Substituted benzoannulated spiroacetals were prepared from (2-haloaryl)alkyl alcohols and dihydropyranyl or dihydrofuranyl pinacol boronates using a Suzuki-Miyaura coupling followed by an acid-catalyzed spirocyclization....
Two previously unreported spiro-cyclopentenones, spirobacillenes A (1) and B (2), were isolated from the 24 h broth culture of Lysinibacillus fusiformis KMC003 derived from acidic coal-mine drainage. The structures of 1 ...
The organocatalytic one-pot oxidative cleavage of terminal 1,2-diols to one-carbon-unit-shorter carboxylic acids is described. The combination of 1-Me-AZADO (cat.), NaOCl (cat.), and NaClO2 caused smooth one-pot oxidativ...
A mild and user-friendly one-pot oxidative cleavage of vicinal diols to their corresponding (di)carboxylic acids using AZADOs and Phl(OAc)(2) is described. 1,2-Diols and 2,3-diols as well as 1,2,3-triol gave one- or two-...
A one-pot synthesis of amides from aldheydes with N-chloroamines, prepared in situ from amines, has been developed. Both aliphatic and aromatic aldehydes and many types of mono- and disubstituted amines are tolerant in t...
Chiral organic anions such as camphorsulfonates and cAMP give rise to the preferential formation of a one-handed helix of an indolocarbazole foldamer, thus inducing characteristic circular dichroic (CD) signals. Moreover...
Chiral phosphoric acid worked together with Hoveyda-Grubbs II catalyst enabling highly efficient synthesis of enantioenriched tetrahydro-beta-carbolines (up to 98% yield, 99% ee) through a ring-closing metathesis/isomeri...
Formal trimerization of the smallest unit of benzyl imidate leads to 2,4,6-tris(benzyloxy)-1,3,5-triazine (TriBOT), which can be used as an acid-catalyzed O-benzylating reagent. The reaction of various functionalized alc...
An unprecedented ruthenium(II)-catalyzed intramolecular oxidative C-N coupling method has been developed for the facile synthesis of a variety of synthetically challenging tri- and tetrasubstituted pyrazoles. Dioxygen ga...
The unconstrained green fluorescence protein (GFP)-like chromophore m-DMABDI displays a high solvatofluorochromicity in aprotic solvents, but the fluorescence is quenched in protic solvents. According to the site-specifi...
Rapid and efficient preparation of peptide thioacids from 2-cyanoethyl peptide thioesters has been accomplished. S-2-Cyanoethyl peptide thioesters were obtained cleanly without the need for purification from resin-bound ...