A copper-catalysed direct radical alkenylation of various benzyl bromides and α-carbonyl alkyl bromides has been developed. Compared with the recent radical alkenylations which mostly focused on secondary or tertiary alkyl halides, this transformation shows good reactivity to primary alkyl halides and tertiary, secondary alkyl halides were also tolerated. The key initiation step of this transfo...

The design and synthesis of a series of alkyl 5(6)-substituted benzimidazole-2-carbamates (1-13), 7-chloro-4-(4-substituted phenyl)aminoquinolines (14-16), 1,2-dimethyl-3-methoxy-carbonyl-4,5-disubstituted pyrroles (17-19) and some compounds belonging to the class pimelonitrile (20), dihydroquinoline (21), pyridine (22), pyridoquinoline (23) and tetrahydro-pyrimidine (24) have been carried out ...

Reaction of pyridinobromocobalt(llI) aetioporphyrin I with a variety of alkyland aryl-magnesium bromides gives the corresponding alkyland aryl-cobalt(lIl) derivatives. In an alternative synthesis, the cobalt(l) derivative of aetioporphyrin J reacts with alkyl or acyl halides to give the alkylor acyl-cobalt(llI) compounds. The latter approach has also been used for the preparation of hydroxyalky...

The susceptibility of the carbonyl group towards nucleophilic attack affords construction various organic compounds. Thus, investigations activation applying greener methodologies are highly important. In present work, among investigated N-halo compounds, N-fluorobenzenesulfonimide (NFSi) has been found as an efficient and selective catalyst in reaction direct esterification aryl alkyl carboxyl...

A series of new N ′ -[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine-4-carbohydrazide derivatives were synthesized. Starting from ethyl piperidine-4-carboxylate (a), first ethyl 1-(phenylsulfonyl)piperidine-4-carboxylate (1), second 1-(phenylsulfonyl)piperidine-4-carbohydrazide (2), and finally N ′ -[(alkyl/aryl)sulfonyl]-1-(phenylsulfonyl)piperidine4-carbohydrazides (4a–n) were synthesized...

The capabilities of porcine pancreatic lipase (PPL), Candida antarctica lipase (CAL), and Candida rugosa lipase (CRL) were evaluated for enantioand/or regioselective acetylation/deacetylation of (±)-2,4-diacetoxyphenyl alkyl ketones, (±)-4-alkyl-3,4-dihydro3-hydroxyalkyl-2H-1,3-benzoxazines, and D-arabino and D-threo-polyhydroxyalkyltriazoles in organic solvents. PPL in tetrahydrofuran (THF) ex...

The conformational analysis of five β-chloroand β-bromo-alkoxides had been done. The minima and the conformational transition states were determined. The anti conformer was found to be the most stable one. Its percentage is more than 99. α-Methylation increases the nuclophilicity of oxygen .Consequently, it enhances the rate of the ring closure. In contrast to βmethylation which retards the rat...

A chromium-catalyzed pinacol-type cross-coupling reaction between alpha,beta-unsaturated carbonyl compounds and aldehydes is reported. Even sterically demanding substrates could be coupled to afford the corresponding pinacols in good yields. Systematic studies concerning the origin of the diastereoselectivities led to the proposal of a mechanism for this synthetically useful reaction. Acroleins...

Several genistein derivatives comprising an isoflavonoid skeleton substituted with an alkyl chain and a sugar moiety show ability to inhibit proliferation of cancer cells in vitro at the concentration several-fold lower than genistein. In our previous studies we shown that these compounds influenced the mitotic spindle, blocked the cell cycle and induced apoptosis. The purpose of this study was...

4-(Alkylamino)carbonyl-1-(alkoxy)carbonyl-2-azetidinones (9-11) have been prepared in five steps from 4-(benzyloxy)carbonyl-1-(t-butyldimethyl)silyl-2-azetidinone (1). The beta-lactam reactivity of 9 has been established by 1H NMR experiment. Compound 11 was a good reversible inhibitor of PPE and HLE. Based on theoretical design, series of 2-azetidinones (12-17) and 4-(alkoxy)carbonyl-2-azetidi...