The study aimed to synthesize and evaluate the potential anti-inflammatory analgesic activities of rationally designed hybrid molecules imidazolone indole nuclei linked through a methylene bridge. Indolyl-imidazolone hybrids were synthesized in three simple steps starting from 2-phenyl-1 H -indole ( 1 ). In first step, compound was converted -indole-3-carbaldehyde 2 ) using standard conditions ...

A Vilsmeier salt supported on solid phase was prepared using piperazine bound to Merrifield resin. Piperazine was selected because it contains two secondary amines: one of the amines is protected upon binding to the resin, and the second was formylated to give resin-1-N-piperazine-4-N-carboxaldehyde (9). Activation of the formamide with either bis(trichloromethyl)carbonate (BTC) or POCl(3) affo...

A variety of novel ligands have been generated by Vilsmeier formylation of Hantzsch pyridines. These compounds which we call DOTTADs contain two aldehyde, imine or amine functions flanking a central pyridine nitrogen and can be homochiral or crown derivatives. The synthesis and manipulation of these systems is discussed. © 2000 Elsevier Science Ltd. All rights reserved. Some years ago we descri...

The key steps in oligosaccharide synthesis are protectinggroup manipulation and stereoselective glycosylation. Various strategies have emerged to expedite glycosylation, and some of these strategies have been elaborated for automated solid-phase synthesis and one-pot cascade glycosylation. Most glycosylation strategies rely on traditional methods for stereochemical control over glycosidic-bond ...

Vilsmeier Several diamide derivatives containing 2-chloroquinoline scaffolds were synthesized via Ugi reaction of 2-chloroquinoline-3-carboxaldehydes, amines, carboxylic acids and isocyanides. The diversity of these quinolinyl Ugi-adducts was increased by using 2-chloroquinoline-3-carboxylic acids as a source of acid. Among them, compounds 2d, 2n, 2p, 4a, 4c and<strong...

The emerging resistance to antimicrobial drugs demands the synthesis of new remedies for microbial infections. Attempts have been made to prepare new compounds by modifications in the quinolone structure. An important method for the synthesis of new quinolone is using Vilsmeier approach but has its own limitations. The present work aimed to synthesize novel norfloxacin analogues using modified ...