A metal-free method for efficient and chemoselective reduction of α-ketoamides using DMF/NaOH/H₂O system has been developed.

A practical and operationally simple hydrodehalogenation of halogenated carboxylic acid derivatives using a DMSO/HCOONa·2H2O system is developed. This protocol avoids the involvement light irradiation, electrochemical apparatus, transition metals, radical initiators, strong bases, other additional additives. Control experiments suggest that HCOONa might function as hydride donor in reduction process via nucleophilic substitution or addition to achieve hydrodehalogenation.

Abstract A series of novel (−)‐1,2,3,9‐tetrahydropyrrolo[2,1‐b]quinazoline‐1‐carboxylic acid derivatives were designed and synthesized. All the prepared compounds screened for their neuroprotective effects using an in vitro oxygen glucose deprivation (OGD) model ischemic stroke. Some target exhibited moderate to excellent protective potency. In particular, 9d , 9e 9g 9h showed significant SH‐SY 5 Y cell line at all three concentrations tested.

A mild and highly diastereoselective one-pot synthesis of trans-N-alkyl-C-nitroaziridines was achieved by treatment nitroalkenes with aliphatic amines N-chlorosuccinimide. Treatment the obtained aziridines a Lewis acid resulted in facile ring opening reaction, accompanied rearrangement isomerization into functionalized (Z)-β-nitroenamines.

Abstract A ruthenium‐catalyzed method has been developed for the C(sp 3 )−H monoborylation of various unactivated alkyl and aryl amides challenging esters, with a low‐cost bench‐stable boron source, providing boronates exclusive selectivity, high efficiency, turnover number (up to 8900). This novel strategy may offer versatile environmentally friendly alternative current methods selective borylation that employ even more expensive metals, such as iridium rhodium.

A catalyst‐ and additive‐free chemoselective transfer hydrogenation of α‐keto amides to α‐hydroxy is easily achieved by using sodium formate as a hydrogen source. The utility this method demonstrated gram‐scale synthesis transformation the resultant into polysubstituted acetamides 2‐arylindole derivatives. Control experiments suggest that NH group crucial for reduction through formation bonds.

This review article introduced synthetic procedures for the preparation of structurally diverse nitroaziridines.In addition, this also summarized reactivity nitroaziridines caused by inherent strain and high electrophilicity small ring.These properties facilitate their use as a functionalized building blocks in medicinal chemistry.

An environmentally benign, highly efficient, and base-promoted selective amination of various polyhalogenated pyridines including the challenging pyridine chlorides to 2-aminopyridine derivatives using water as solvent has been developed. Featuring use new method, reaction is extended transformation on a large scale. Mechanistic studies indicate that pathway involving base aidant dissociation N,N-dimethylformamide generate dimethylamine likely.

The first hydride-catalyzed reductive cleavage of tertiary amides using the hydrosilane as reducing reagent has been developed. This transition-metal-free process may offer a versatile alternative to current systems for selective amides.

Bis(functionalization), 4-alkoxylation and 3-chlorination, of the 1-methyl-2-quinolone framework was achieved under mild conditions by a sequential treatment 3-nitrated 1-methyl-2-quinolones with sodium alkoxide N-chlorosuccinimide. Moreover, succinimide group instead an alkoxy introduced at 4-position, affording masked form 4-amino-3-chloro-2-quinolone derivative. Furthermore, prepared vicinally functionalized quinolones thus obtained were subjected to Suzuki-Miyaura coupling reaction,...

Abstract Six‐ or seven‐membered dibenzosultams were synthesized upon treatment of N ‐aryl‐ ‐benzyl‐2‐halobenzenesulfonamides with HCOONa ⋅ 2H 2 O in DMSO without using additional measures and additives, such as light irradiation, electrochemical apparatus, transition metals, oxidants. Further functionalization the free NH group resultant demonstrates synthetic practicability this method. magnified image

We report the preparation of symmetrical bis(indolyl)acetamides using dimerization 2-hydroxy-(2-indolyl)acetamides and unsymmetrical via electrophilic substitution indoles with 2-hydroxy-(2-indolyl)acetamides.Both conversions were mediated by protic acid in THF at room temperature.

A direct alkoxy-dihalogenation method of nitroalkenes was developed by a three-component reaction using alcohol and <italic>N</italic>-halosuccinimide.

A method for chemoselective reduction of α‐keto amides and esters using tosylhydrazine in the presence NaHCO3 has been developed. variety α‐hydroxy were obtained good to excellent yields, demonstrating efficiency present protocol. possible reaction mechanism is proposed based on deuterium‐labelling experiments.

Abstract A catalyst‐ and additive‐free synthesis of α‐pyrrolyl amides was easily achieved upon treatment 4‐hydroxy‐L‐proline with α‐keto amides. Broad substrate scope, good functional group tolerance, operational simplicity are the notable advantages this protocol. Furthermore, gram‐scale further transformation resultant products into newly functionalized compounds definitely demonstrated synthetic utility method.

Abstract A novel cobalt‐catalyzed reduction of 2‐pyridyl ketones and related heteroaryl compounds using formate as reductant was developed. Ketone substrate is activated by chelation with cobalt, which makes the present method highly selective. possible reaction mechanism proposed.

A method for chemoselective reduction of 2-pyridyl ketones and related N-heteroaryl compounds catalyzed by cobalt stearate using DMF as a hydride source is developed. The ketone substrate activated chelation with cobalt, which makes the present highly chemoselective. possible reaction mechanism proposed on basis control experiments.

Usual 1-methyl-2-quinolone (MeQone) derivatives are not reactive due to aromatic property, and direct functionalization of the MeQone framework hardly occurs. On other hand, a nitro group is considered be useful activating for this that enables concise chemical transformation. In present work, 4-alkoxylation 3-halogenation easily achieved by sequential treatment 3-nitrated MeQones with sodium alkoxide N- halosuccinimide. Moreover, regioselective C-C bond formation at 4-position treating...

Direct aziridination of a nitrostyrene is achieved upon treatment with an alkylamine and N-chlorosuccinimide. The reaction initiated by the Michael addition amine to nitroalkene. Subsequent N-chlorination nucleophilic substitution at nitrogen atom afford 1-alkyl-2-nitroaziridine diastereoselectively. This mechanism was clarified NMR studies.

Abstract Dimerization of hydroxyindolylacetamides (I) and (V) leads to formation symmetrical bis(indolyl)acetamides (II) (VI), resp., while electrophilic substitution indoles (III) (VII) with indolylacetamides give rise unsymmetrical (IV) (VIII).

Abstract Some of the synthesized compounds show moderate to excellent protective potency in screening for their neuroprotective effects.