A novel and efficient PhI(OAc)2-promoted one-pot reaction of aromatic hydroxylamines, aldehydes, and TMSCN in the presence of BF3·Et2O is described. A wide variety of N-substituted benzimidazolones are obtained with satisfactory yields under mild reaction conditions. The method was proven to be efficient for the synthesis of benzimidazolone derivatives from readily available starting materials.

A facile and efficient synthesis of N-acetoxy-N-arylamides through double acylations of hydroxylamines with aldehydes and diacetoxyiodobenzene is reported. The yields of the products are good to excellent.

A highly efficient [3 + 2] cycloaddition between trifluoromethylated N-acylhydrazones and nitroolefins in the presence of potassium hydroxide under phase transfer catalysis is developed to afford potentially bioactive trifluoromethylated pyrazolidines, which can be further transformed into trifluoromethylated pyrazoles in good yields.

Cheap and commercially available trichloroisocyanuric acid has been used to promote trifluoromethylation by using TMSCF3 as the trifluoromethyl source. The method provides a novel and efficient protocol for the construction of CF3-containing 4,5-dihydroisoxazoles from allylic oximes in good to excellent yields.

An efficient and convenient one-pot method for the preparation of trifluoromethylated homoallylic N-acylhydrazines or α-methylene-γ-lactams has been described. In this process, allyl bromide and metal tin are used instead of toxic stannanes, and commercially available aqueous trifluoroacetaldehyde methyl hemiacetal was used as a trifluoromethyl source.

•A new kind of mono-oxazoline ligands was prepared.•The ligands combined diaryl methyl units and chiral oxazoline ring together.•Pyridine ring was used as the linker of the two units.•The ligands were applied in the enantioselective electrophilic fluorination of β-ketoesters.•Moderate ee values were obtained.A new kind of mono-oxazoline ligands which combined diaryl methyl units and chiral oxazoline units together using pyridine as linker was prepared. Their applications in enantioselective electrophilic fluorination of β-ketoesters by NFSI were investigated, and the corresponding products were obtained in excellent yield (up to 90%) and good enantioselectivity (78%) in CH2Cl2 at −60 °C.Enantioselective electrophilic fluorination of β-ketoesters by NFSI was investigated by using new kind of chiral mono-oxazoline ligands (L1–L6), and moderate to good ee value were obtained.

A concise and efficient method for the synthesis of α-methylene-γ-lactams is developed from multicomponent one-pot reactions of aldehydes or ketones, hydrazides, and ethyl 2-(bromomethyl)acrylate promoted by tin powder. The reaction proceeds smoothly under mild reaction conditions without using any catalyst to give the corresponding products in high yields. α-Methylene-γ-spirolactams can also be prepared from cyclic ketones.

2,5-Disubstituted tetrahydrofurans were obtained from lactones and organozinc halides in moderate to high yield in the presence of Lewis acids.

A powerful reagent, P[NCH3(OCH3)]3 (3), for conversion of carboxylic acids directly to Weinreb amides was developed. In most cases the yields of the corresponding Weinreb amides were above 90% when P[NCH3(OCH3)]3 was heated with aromatic and aliphatic carboxylic acids in toluene. The sterically hindered carboxylic acids can also give the corresponding Weinreb amides in excellent yields.

A concise, efficient and direct trifluoromethylation method of aldehyde-derived N-acylhydrazones has been firstly developed by using the combination of inexpensive, stable and commercially available TMSCF3 and PhI(OAc)2 as the CF3 source under mild reaction conditions. This method provides easy access to highly functionalized trifluoromethylated N-acylhydrazones, which could be used as trifluoromethyl synthetic building blocks to be further transformed into other valuable trifluoromethyl compounds.

A facile and efficient synthesis of N-acetoxy-N-arylamides through double acylations of hydroxylamines with aldehydes and diacetoxyiodobenzene is reported. The yields of the products are good to excellent.

A highly efficient [3 + 2] cycloaddition between trifluoromethylated N-acylhydrazones and nitroolefins in the presence of potassium hydroxide under phase transfer catalysis is developed to afford potentially bioactive trifluoromethylated pyrazolidines, which can be further transformed into trifluoromethylated pyrazoles in good yields.

An efficient and convenient one-pot method for the preparation of trifluoromethylated homoallylic N-acylhydrazines or α-methylene-γ-lactams has been described. In this process, allyl bromide and metal tin are used instead of toxic stannanes, and commercially available aqueous trifluoroacetaldehyde methyl hemiacetal was used as a trifluoromethyl source.