Gonghua Song

Pd-Catalyzed Csp2H Functionalization of Heteroarenes via Isocyanide Insertion: Concise Synthesis of Di-(Hetero)Aryl Ketones and Di-(Hetero)Aryl Alkylamines

We report herein an efficient Pd-catalyzed direct C-H bond functionalization of heteroarenes via an isocyanide insertion strategy for the synthesis of di-(hetero)aryl ketones and di-(hetero)aryl alkylamines. The methodology involves a three component reaction between an azole, a haloarene and an isocyanide resulting in the formation of an imine, which in turn is either hydrolyzed or reduced to get the desired product.

Microwave-Assisted Copper-Catalyzed Oxidative Cyclization of Acrylamides with Non-Activated Ketones.

An operationally simple and efficient microwave-assisted protocol for the oxidative cyclization of acrylamide derivatives with non-activated ketones to generate 3,3-disubstituted oxindoles is described. The reaction proceeds by a copper-catalyzed tandem radical addition/cyclization strategy and tolerates a series of functional groups with moderate to excellent yields.

Nano Cu-catalyzed efficient and selective reduction of nitroarenes under combined microwave and ultrasound irradiation

In situ preparation of copper nanoparticles from a copper acetate precursor and its application as an efficient catalyst for the selective reduction of aromatic nitro compounds with hydrazine hydrate under combined microwave and ultrasound irradiation were described in detail. The results reveal the synergetic effect of microwave and ultrasound on the synthesis of copper nanoparticles, and formation of various amino derivatives.

Novel Fused Heterocycles: Synthesis and Activity of 5,6-Dihydro-7-thia-1,3,3a,5-tetraazainden-4-one and 1-Thia-3,4a,9-triazafluoren-4-one Derivatives

Summary. Thiatetraazaindenone derivatives were synthesized by reaction of 3-substituted 1,2,4-triazole-5-thiols with N-substituted N-chloromethyl carbamoyl chlorides. A series of thiatriazafluorenone derivatives were also prepared by reaction of benzimidazole derivatives with the same substrate. Some of the new compounds show fungicidal, herbicidal, and insecticidal activity.

A simple and efficient synthesis of fused morpholine pyrrolidines/piperdines with potential insecticidal activities

A simple and efficient synthesis of fused morpholine pyrrolidine/piperdine core structures was accomplished via a Petasis-borono Mannich reaction of cyclic amino alcohols, glyoxal and arylboronic acids with moderate to good yields. The bioassay data showed that the synthesized compounds displayed selective insecticidal activities against armyworm and root-knot nematode.

FeCl3-promoted synthesis of 1,3,4-thiadiazoles under combined microwave and ultrasound irradiation in water

An eco-friendly and efficient synthesis of substituted 1,3,4-thiadiazole derivatives has been developed. This aqueous heterogeneous approach proceeds smoothly and quickly under combined microwave and ultrasound irradiation in the presence of FeCl3.Graphical Abstract

Direct C-2 acylation of indoles with toluene derivatives via Pd(II)-catalyzed C–H activation

A simple and efficient Pd-catalyzed method for the C2-acylation of indoles is described. Less toxic, stable, and commercially available toluene derivatives were used as acyl sources, with tert-butylhydroperoxide (TBHP) as oxidant and pivalic acid as additive, providing moderate to good yields.

Solid phase synthesis of aminochalcones

A microwave-assisted solid phase synthesis of aminochalcones via the Claisen–Schmidt condensation reaction between resin-bound p-aminoacetophenone and aromatic aldehydes was described.

One-pot three-step synthesis of 3-aryl-2-benzoylimino-4-thiazolidinones in the ionic liquid [bmim+][PF6-]

3-Aryl-2-acylimino-4-thiazolidinones are efficiently formed in 1-n-butyl-3-methylimidazolium hexafluorophosphate [bmim][PF6] as solvent in a one-pot three-step procedure. The ionic solvent could be recovered and recycled four times with no diminution in yields.