Discovery of novel 1,2,4-triazole schiff bases hybridized with 1,4-naphthoquinones as potent STAT3 inhibitors.

Signal transducer and activator of transcription 3 (STAT3) is closely related to a variety of cancers. The research of novel STAT3 inhibitors is an important and meaningful project for pharmaceutical chemist. In this study, 10 novel 1,4-naphthoquinones carrying 1,2,4-triazole derivatives were synthesized via a four-step synthesis starting from 2-hydroxynaphthalene-1,4-dione.

Cobalt-Catalyzed Cross-Coupling of Glycosyl Sulfones with Zinc reagents toward the Stereoselective Synthesis of C(sp/sp)-Glycosides.

A cobalt-catalyzed desulfonylative cross-coupling of glycosyl sulfones with organozinc reagents toward the stereoselective synthesis of C-glycosides is reported. The new C-glycoside synthesis proceeds under mild reaction conditions and exhibits tolerance to a range of functional groups. Diverse alkynylated, arylated, and alkenylated products are formed with high efficiency and excellent diastereoselectivity.

Stereoretentive Conversion to -Glycosides from -Glycosides via Ligand-Coupling on Sulfur(IV).

A novel strategy is reported for the stereoselective synthesis of C(sp)-C(sp) -glycosides, which converts heteroaryl -glycosides into heteroaryl -glycosides with retention of configuration through a sequential process involving oxidation and Grignard reagent attack. The new method involves the generation of a S(IV) intermediate, followed by ligand coupling of the glycosyl and heteroaryl groups to yield heteroaryl -glycosides. The diverse heteroaryl -glycosides were achieved with good efficiency.

Cp*Rh(III)-catalyzed regioselective cyclization of aromatic amides with allenes.

A new Cp*Rh(III)-catalyzed regioselective cyclization reaction of aromatic amides with allenes is reported. The use of allenyl derivatives bearing a directing-group assistant as a reaction promoter was the key to the success of this protocol. In this catalytic system, -(pivaloyloxy)benzamide substrates react with allenes Rh-σ-alkenyl intermediates, while -(pivaloyloxy) indol substrates react Rh-π-allyl intermediates.