Deaminative carbonylative thioesterification of activated alkylamines with thiophenols under transition-metal-free conditions
A transition-metal-free radical carbonylation of activated alkylamines with thiophenols has been successfully developed. Various thioesters were selectively produced with moderate to good yields.
One-pot three-component reaction of p-quinone monoacetals, L-proline and naphthols to afford N-aryl-2-arylpyrrolidines
A one-pot three-component reaction of p-quinone monoacetals (or p-quinol ethers), L-proline and naphthols is developed for the synthesis of N-aryl-2-arylpyrrolidines under mild conditions with high chemo- and regioselectivity.
Mechanistic insights into the Rh(I)-catalyzed transannulation of 1,2,3-thiadiazoles with alkenes, alkynes, and nitriles: Does the intermediacy of α-thiavinyl Rh-carbenoids play an important role?
Density functional theory (DFT) calculations were performed to gain an in-depth mechanistic understanding of the Rh(I)-catalyzed transannulation of 1,2,3-thiadiazoles with alkenes, alkynes, and nitriles.
Diastereoselective construction of cage-like and bridged azaheterocycles through dearomative maximization of the reactive sites of azaarenes
A highly diastereoselective multicomponent dearomative multifunctionalization of N-alkyl activated azaarenes with 1,5-diazapentadienium salts has been developed to access structurally rigid and synthetically challenging cage-like and bridged azaheterocycles.
Total and formal syntheses of fostriecin
Two formal syntheses and one total synthesis of fostriecin (1) have been achieved, as well as, the synthesis of its related congener dihydro-dephospho-fostriecin.
Enantioselective copper-catalysed defluorosilylation of trifluoro-methylated alkenes with silylboronates
An efficient method for the construction of gem-difluoroallylsilanes with high enantiomeric excess via a copper-catalysed defluorosilylation of trifluoromethylated alkenes with silylboronates is described.
(2-Ketulosonyl)onate 2,3-O-thionocarbonate donors for the synthesis of KO and KDO α-glycosides and a one-pot glycosylation method for 2-keto acid donors
Bifunctional (2-ketulosonyl)onate thionocarbonates are effective donors for the synthesis of KO and KDO α-glycosides with perfect control in stereoselectivity.
Oxidative cascade cyclization of 2-cyano-3-arylaniline derived acrylamides with toluenes, ethers, aliphatic alcohols or simple alkanes
Oxidative radical cascade cyclization of 2-cyano-3-arylaniline derived acrylamides with a variety of hydrocarbons including toluenes, ethers, aliphatic alcohols and alkanes has been developed to construct alkyl substituted pyridophenanthridines.
Access to SCN-containing thiazolines via electrochemical regioselective thiocyanothiocyclization of N-allylthioamides
An electrochemical thiocyclization of N-allylthioamides has been developed for the synthesis of SCN-containing 2-thiazolines and NCS-containing thiazines.
One-pot chemoselective domino condensation to form a fused pyrrolo–pyrazino–indolizine framework: discovery of novel AIE molecules
A fused pyrrolo–pyrazino–indolizine (5-6-6-5) framework with excellent AIE properties and application in living cell imaging was constructed via chemoselective domino condensation.
Transition-metal-free aerobic C–O bond formation via C–N bond cleavage
We disclosed a TM-free cascade SNAr-[3,3] rearrangement–rearomatization process for the efficient construction of NOBIN-type biaryls from readily available (hetero)arylhydroxylamines and aryltrimethylammonium salts under mild conditions.
Discovery of highly functionalized 5,6-seco-grayanane diterpenoids as potent competitive PTP1B inhibitors
Three competitive PTP1B inhibitory diterpenoids with a 5,6-seco-grayanane carbon skeleton (1–3) were isolated and identified from Rhododendron molle. A more potent competitive PTP1B inhibitor (9) was designed and prepared based on a docking study.
Cocrystallization with a clip-type molecule catcher: a new method to determine structures of liquid molecules
In order to measure the precise structure of liquid molecules by X-ray single-crystal diffraction, we report a new and easy method using a glycoluril-derived molecular clip as a molecule catcher to form cocrystals with liquid molecules.
Efficient labeling of organic molecules using 13C elemental carbon: universal access to 13C2-labeled synthetic building blocks, polymers and pharmaceuticals
Synthetic methodology enabled by 13C-elemental carbon is reported. Calcium carbide Ca13C2 was applied to introduce a universal 13C2 unit in the synthesis of labeled alkynes, O,S,N-vinyl derivatives, labeled polymers and 13C2-pyridazine drug core.