Treating 2-chloro-4-(4-chlorophenyl)-6-methylbenzo[d]-3,1-oxazinium hexachloroantimonate (1) with one equivalent of alcohol or mercaptane led, after hydrolysis with aq. NaOH, to the formation of 4,4-disubstituted-1,4-dihydro-2H-6-methyl-3,1-benzoxazin-2-ones (3). Large excess addition of alcohol afforded either 4’-chloro-2-isocyanato-5-methylbenzophenone disubstitutedketal (4) or N-{2[(4-chloro...

In the title compound, C(17)H(18)N(4)O(3)·C(3)H(7)NO, the main disubstituted urea and solvate mol-ecules are linked by pairs of N-H⋯O hydrogen bonds. In the main mol-ecules, the benzene rings form a dihedral angle of 15.59 (13)° a;nd two intra-molecular O-H⋯N hydrogen bonds influence the mol-ecular conformation. In the crystal structure, weak inter-molecular C-H⋯O inter-actions link the hydroge...

Several methods have been reported for the syn­ thesis of isocyanates, most of them involving the use of phosgene: e.g. phosgene and primary amines [1] either in basic [2] or in acidic medium [1]; phosgene and diaryl urea [1]; phosgene and l-alkyl-3-arylsulphonyl urea [3]; or phosgene and sulfinyl amines [4], Isocyanates were further synthesized from olefins or alkyl halides by the use of isocy...

Soluble epoxide hydrolase enzyme is a promising therapeutic target for hypertension, vascular inflammation, pain and some other risk factors of cardiovascular diseases. The most potent sEH inhibitors reported in the literature are urea-based ones which often have poor bioavailability. In this study, in a quest for finding potent inhibitors of soluble epoxide hydrolase, some 4,6-disubstituted py...

Soluble epoxide hydrolase enzyme is a promising therapeutic target for hypertension, vascular inflammation, pain and some other risk factors of cardiovascular diseases. The most potent sEH inhibitors reported in the literature are urea-based ones which often have poor bioavailability. In this study, in a quest for finding potent inhibitors of soluble epoxide hydrolase, some 4,6-disubstituted py...

Tandem reactions involving Rh-catalyzed intermolecular hydroacylations of alkynes with salicylaldehydes followed by intramolecular oxo-Michael additions are described for the diastereoselective synthesis of 2,3-disubstituted chroman-4-ones. The tandem hydroacylation/oxo-Michael additions occur to form 2,3-disubstituted chroman-4-ones in high yields from a range of 1,2-disubstituted acetylenes a...

The inhibition of the mammalian soluble epoxide hydrolase (sEH) is a promising new therapy in the treatment of hypertention and inflammation. The problems of limited water solubility and high melting points commonly displayed by the active 1,3-disubstituted ureas prevent the further development of potent urea-based sEH inhibitors. Therefore, a new class of potent inhibitors of sEH were designed...

A new class of inhibitors of juvenile hormone epoxide hydrolase (JHEH) of Manduca sexta and further in vitro characterization of the enzyme are reported. The compounds are based on urea and amide pharmacophores that were previously demonstrated as effective inhibitors of mammalian soluble and microsomal epoxide hydrolases. The best inhibitors against JHEH activity so far within this class are N...

A series of multidentate N-donor ligands have been synthesised all containing pyridyl and pyridyl/thiazole units and their coordination behaviour is described. The ligands are classified into four types; i) terpyridine containing pyridyl/thiazole ligands (L); ii) pyridyl/thiazole ligands containing a 3,3′-disubstituted bipyridine core. (L); iii) 2,2′-bipyridine containing a crown ether moiety (...