1- (Phthalazin-l'-yl-amino)-3-chloro-4-aryl-4H-(4o-rm ethyl)-2-azetidinones (3) were prepared by cycloaddition of-methyl substituted benzal hydrazinophthalazine (2) with chloro acetylchloride. The hydrazone (2) was synthesised by the condensation of 1- hydrazinophthalazine (1) with substituted aromatic aldehydes, ketones 7 acetophenones. 1- Hydrazinophthalazine was prepared from the phthal...

The Brønsted-acidic ionic liquid 1-methyl-3-(4-sulfobutyl)imidazolium triflate [BMIM(SO(3)H)][OTf] was demonstrated to act efficiently as solvent and catalyst for the halogenation of activated organic compounds with N-halosuccinimides (NXS) under mild conditions with short reaction times. Methyl aryl ketones were converted into α-halo and α,α-dihaloketones, depending on the quantity of NXS used...

A novel and convenient copper (II) bromide and 1,8-diazabicyclo[5.4.1]undec-7-ene (DBU) or 1,10-phenanthroline catalysis protocol for the construction of α-alkyl-β-keto sulfones via C(sp(3))-H bond functionalization followed by C(sp(3))-S bond formation between aryl ketones and sodium sulfinates at room temperature has been developed. This method is applicable to a wide range of aryl ketones an...

A slight excess of silyl trifluoromethanesulfonate mediates a tandem enol silane formation-Mukaiyama aldol reaction in the presence of Hunig’s base. Preformation of the enol silane is unnecessary for efficient reactions, which proceed in 75-97% yield for the addition of aryl methyl ketones and acetate esters to non-enolizable aldehydes. Mechanistic data suggests that free amine is crucial for f...

A simple, efficient and practical copper-catalyzed aerobic oxidative synthesis of α-ketoamides from aryl methyl ketones, aliphatic amines and N-iodosuccinimide (NIS) has been developed. The one-pot reaction may proceed smoothly at room temperature in the open air. The possible mechanism for the formation of α-ketoamides was proposed. Molecular oxygen in air functions as both an oxidant and an o...

1- (phthalazin-l'-yl-amino)-3-chloro-4-aryl-4h-(4o-rm ethyl)-2-azetidinones (3) were prepared by cycloaddition of-methyl substituted benzal hydrazinophthalazine (2) with chloro acetylchloride. the hydrazone (2) was synthesised by the condensation of 1- hydrazinophthalazine (1) with substituted aromatic aldehydes, ketones 7 acetophenones. 1- hydrazinophthalazine was prepared from the phthal...

The first allylic carbonylation reaction of allylic acetates with aryl boronic acids under carbon monoxide has been developed. Using Pd-PCy3 as a catalyst, a wide spectrum of allylic acetates was carbonylated in the presence of various aryl boronic acids, affording α,β-unsaturated aryl ketones in good to excellent yields. Preliminary studies indicate that carbon monoxide always inserts at the l...

Benzoyl radicals are generated directly from (hetero)aromatic aldehydes upon tetrabutylammonium decatungstate ((n-Bu(4)N)(4)W(10)O(32)), TBADT) photocatalysis under mild conditions. In the presence of alpha,beta-unsaturated esters, ketones and nitriles radical conjugate addition ensues and gives the corresponding beta-functionalized aryl alkyl ketones in moderate to good yields (stereoselective...

A one-pot, three-step protocol for the preparation of Grignard reagents from organobromides in a ball mill and their subsequent reactions with gaseous carbon dioxide (CO2) or sodium methyl carbonate providing aryl alkyl carboxylic acids up to 82 % yield is reported. Noteworthy are short reaction times significantly reduced solvent amounts [2.0 equiv. liquid assisted grinding (LAG) conditions]. ...