Nucleophilic substitution reactions of 2-halo-2H-azirines 1a, 1b, 1d, and 1e with potassium phthalimide and aniline allowed the preparation of new substituted 2H-azirines 2-5. The reactions of 2-bromo-2H-azirine 1a with methylamine led to the synthesis of alpha-diimines 7 and 8. 2-Halo-2H-azirines were also established as building blocks for the synthesis of a range of heterocyclic compounds, n...

Iridium- and ruthenium-free approaches to protected allylic amines and alkyl nitriles under photoredox conditions are reported. An inexpensive organic dye, eosin Y, catalyzes coupling of Boc-protected potassium α-aminomethyltrifluoroborates with a variety of substituted alkenyl sulfones through an α-aminomethyl radical addition-elimination pathway. Allylic and homoallylic amines were formed in ...

The title compound, C(12)H(8)N(2)O(5), was obtained by the reaction of 1-chloro-2,4-dinitro-benzene and phenol in the presence of potassium carbonate. The nitro-substituted benzene ring lies on a mirror plane, with one NO(2) group in the same plane and the other disordered across this plane. The phenoxy-benzene unit is placed perpendicular to this mirror, resulting in an exact orthogonal relati...

In continuation of our search for new substituted pyridine based anti-inflammatories, reaction of 1-(2-thienyl or furanyl)-3-(2-hydroxyphenyl)-2-propen-1-ones (1) with malononitrile in alcoholic KOH solution afforded a mixture of 4-alkoxy-2-(2-thienyl or furanyl)-5H-[1]benzopyrano[3,4-c]pyridine-5-ones (2) and 2-alkoxy-4-amino-6- (2-thienyl or furanyl)-3,5-pyridinedicarbonitriles (3). Some of t...

A series of 1-substituted 2, 4, 5 triphenyl imidazoles were synthesized by the reaction equimolar mixture of 2, 4, 5 triphenyl imidazole with chloro compound in the presence of anhydrous potassium carbonate. The newly synthesized compounds were characterized on the basis of UV, IR and H NMR spectra. The synthesized compounds were screened for antiinflammatory, antimicrobial activities. Antiinfl...

Anilines 1a-h on reaction with potassium thiocyanate and bromine in acetic acid yielded substituted 2-amino[2,1-b][1,3]benzothiazoles 3a-h. The compounds 3a-h on reaction with ethyl acetoacetate and pheylidine acetoacetate, yielded, 2-methyl-4-H-pyrimido[2,1b][1,3]benzothiazole-4-ones 4a-h and ethyl 4-phenyl-2-methyl-4H–pyrimido[2,1b][1,3]benzothiazole-3-carboxylates 5a-h respectively. Pheylidi...

cholamines. JOEL G. HARDMAN AND STEVEN E. MAYER 29 Antagonism of Monoamine Oxidase Inhibitors against Norepinephrine, Acetyicholine and Potassium in the Isolated Nictitating Membrane of the Cat. T. H. TSAI AND W. W. FLEMING 40 A St.udy of the Potentiation of Tryptamine by Monoamine Oxidase Inhibitors in the Dog. JOHN NELSON EBLE 48 Pharmacology of a Group of Phenylpiperazine Tetrazole Derivativ...

The synthesis of 2-(chloromethyl)-2,1-borazaronaphthalene has provided an opportunity to expand dramatically the functionalization of the azaborines. This azaborinyl building block can serve as the electrophile in palladium-catalyzed cross-coupling reactions to form sp(3)-sp and sp(3)-sp(2) bonds. The cross-coupling reactions of 2-(chloromethyl)-2,1-borazaronaphthalene with potassium (hetero)ar...

The general lipid-lowering action of the N-substituted phthalimide derivatives reported herein, as well as the activity of potassium phthalimide, implicates the phthalimide moiety as possessing hypolipidemic activity in rodents. Compounds containing substituents with chain lengths of four carbon or oxygen atoms showed the best hypolipidemic activity in the series tested. Tests involving 1-N-pht...

cholamines. JOEL G. HARDMAN AND STEVEN E. MAYER 29 Antagonism of Monoamine Oxidase Inhibitors against Norepinephrine, Acetyicholine and Potassium in the Isolated Nictitating Membrane of the Cat. T. H. TSAI AND W. W. FLEMING 40 A St.udy of the Potentiation of Tryptamine by Monoamine Oxidase Inhibitors in the Dog. JOHN NELSON EBLE 48 Pharmacology of a Group of Phenylpiperazine Tetrazole Derivativ...