A novel iodine promoted [1 + 3 2] cleavage cyclization reaction for the synthesis of 1 H -pyrazolo[3,4- b ]pyridines from aryl methyl ketones, 5-aminopyrazoles and enaminones has been established.

A [3 + 1 2] cyclization–rearrangement reaction scheme was developed to synthesize pyrimido[1,2-b]indazoles from aryl methyl ketones, 3-aminoindazoles, and gem-diarylethenes. This metal-free process proceeds via a sequential aza-Diels–Alder Wagner–Meerwein rearrangement, possible mechanism demonstrated based on control experiments. method exhibits good substrate compatibility allows simple conditions. Moreover, the products display significant aggregation-induced emission characteristics...

An unprecedented dual α,β-C(sp 2 )–H functionalization/bicyclization strategy of o -hydroxyphenyl enaminones for the preparation chromeno[2,3- b ]pyrrol-4(1 H )-ones has been established.

Quinazoline skeletons are synthesized by amino acid catabolism/reconstruction combined with the insertion/cyclization of dimethyl sulfoxide for first time.

A novel multicomponent cascade cyclization reaction in one pot for the preparation of pyrido[3,2-a]phenoxazin-5-ones from simple o-aminophenols, paraformaldehyde, and enaminones has been established. It is noteworthy that o-aminophenol plays multiple roles serving as both a bis-nucleophile an iminoquinone precursor, which can situ generate aminophenoxazinones to undergo Povarov first time yield with high efficiency. Moreover, photoluminescence polarity sensitivity features...

A novel I2-mediated Povarov reaction of arylacetylenes and anilines for the synthesis 2,4-substituted quinolines has been developed, in which arylacetylene first acts as both a diene precursor dienophile. This work further develops to expand types precursors. Preliminary mechanistic studies indicate that I2/DMSO system realized oxidative carbonylation C(sp)–H then undergoes [4 + 2] cycloaddition reaction.

A novel multicomponent cascade cyclization and sulfenylation/selenation using aryl methyl ketones, isoquinolin-1-amine, sodium arylsulfinates/1,2-diphenyldiselane to synthesize imidazo[2,1-a]isoquinoline derivatives in one-pot via the construction of two C-N bonds one C-S/C-Se bond has been reported. This reaction realizes simultaneous C(sp3)-H amination sulfenylation/selenation, avoiding complicated prior substrate preparation. process simple operating conditions good compatibility.

An I 2 –DMSO mediated one-pot approach to imidazo[2,1- a ]isoquinoline derivatives from readily available aryl methyl ketones and isoquinolin-1-amine has been demonstrated.

Abstract A I 2 ‐DMSO mediated approach to introduce −OCD 3 into pyrroles in situ via multicomponent cascade cyclization reaction using methyl ketones, aniline, ethyl benzoylacetate and CD OD as readily available substrates is reported. This process realizes introduction of the Hantzsch pyrrole synthesis deuterated alkoxy‐substituted with formation one C−C bond, C−O bond two C−N bonds pot. Notably, this conversion has good substrate compatibility (62 examples) eliminates need for anhydrous...

Nuclear factor- κB (NF- κB) plays a pivotal role in the regulation of immune and inflammatory responses. The real-time expression level NF- reflects development ulcerative colitis (UC). Polydatin has vast pharmacological activities, including inhibiting production mediators, inducing antioxidants, regulating function, etc. purpose this study was to investigate potential inhibitory effects polydatin on pathway activation mouse UC model. results showed that treatment downregulated p65 activity...

We herein report an iodine-mediated formal [2 + 2 1] cyclization of methyl ketones, p-toluenesulfonyl hydrazines, and 1-aminopyridinium iodide for preparation 4-aryl-NH-1,2,3-triazoles under metal- azide-free conditions. Notably, this is achieved using hydrazines as azide surrogates, providing a novel route toNH-1,2,3-triazoles. Furthermore, approach provides rapid practical access to potent inhibitors indoleamine 2,3-dioxygenase (IDO).

A novel [2 + 1 3] cyclization reaction for the synthesis of 2-aryl-4-quinolinecarboxylates from aryl methyl ketones, arylamines, and 1,3-dicarbonyl compounds has been established. This metal-free process achieved C–C bond cleavage directly as a single-carbon synthon. The is highly efficient good substrate compatibility while operating under mild conditions. method practicability successfully realized bioactive molecules.

In this paper, novel sulfur-containing 1,6-dihydrofuro[3,2-

A novel iodine promoted cyclization of enaminone with aryl methyl ketones has been developed as a straightforward method for constructing 2-hydroxy-pyrrol-3(2H)-ones. This strategy affords structurally diverse 2-hydroxy-pyrrol-3(2H)-ones rings in high yields. Moreover, quarternary alcohol constructed efficiently the reaction. Product purification required only washing CH2Cl2 solvent, thereby avoiding traditional chromatography and recrystallization, making this an example group-assisted chemistry.

2-Hydroxy-4-morpholin-2,5-diarylfuran-3(2H)-one derivatives were constructed sequentially using iodine and zinc dust from simple readily available methyl ketone morpholine as the starting materials. Under mild conditions, C–C, C–N, C–O bonds formed in a one-pot synthesis. A quaternary carbon center was successfully constructed, active drug fragment introduced into molecule.

A novel [3 + 1 1] cyclization reaction for the synthesis of compounds based on a 5-cyano-1 H -pyrazolo[3,4- b ]pyridine skeleton from aryl methyl ketones, malononitrile and 5-aminopyrazoles has been established.

Comprehensive Summary A [2 + 1 1] cyclization reaction has been developed for the synthesis of multisubstituted β ‐pyrrolidinones from commercially available aryl methyl ketones, primary amines, and ethyl nitroacetate. In this I 2 –DMSO‐meditated process, C—NO bond nitroacetate is cleaved, affording a C1 synthon, formation two C—C C—N bonds quaternary carbon center are constructed in one pot. This method good substrate compatibility permits late‐stage modification pharmaceutical compounds.

Skeleton editing for heteroarenes, especially pyrazoles, is challenging and remains scarce because these non-strained aromatics exhibit inert reactivities, making them relatively inactive performing a dearomatization/cleavage sequence. Here, we disclose cycloaddition-induced scaffold hopping of 5-hydroxypyrazoles to access the pyrazolopyridopyridazin-6-one skeleton through single-operation protocol. By converting five-membered aza-arene into five-unit spine 6/6 fused-bicyclic, this work...

We herein report an I2/CuCl2-copromoted diamination of C(sp3)-H bonds for the preparation 2-acyl-4-aminoquinazolines from methyl ketones, 2-aminobenzonitriles, and ammonium acetate. This reaction features operational simplicity, commercially available substrates, mild conditions, good functional group compatibility. Mechanistic studies indicate that CuCl2 plays a pivotal role in this transformation. study uses as novel input to construct 2-acyl-4-aminoquinazoline derivatives first time.

A reductive coupling reaction was established for the synthesis of diaryl 1,2-dicarbonyl compounds from aryl methyl ketones in good yields. The mechanistic study showed undergoes C(CO)–C(sp3) bond cleavage, with occurring through an electron transfer process. Notably, not only is simple to operate but also has mild conditions and a wide range applicable substrates.

A novel process using N-benzylhydroxylamine hydrochloride as a “C1N1 synthon” in [2 + 2 1] cyclization for the construction of 1,2,5-trisubstituted imidazoles has been described first time. The key to realizing this lies on capturing arylamines by situ generated acyl ketonitrone intermediates. Subsequent tautomerization activates α–C(sp3)−H N-benzylhydroxylamines, thus breaks through its inherent reaction mode and achieves N, α–C site-selective cyclization. Furthermore, method enables...

We report an unconventional I