A hydrazine-free Wolff–Kishner reaction suitable for an undergraduate laboratory [PDF]
A Wolff–Kishner reaction that does not require hydrazine has been developed. The reaction sequence has two steps; formation of a carbomethoxyhydrazone from methyl hydrazinocarboxylate and acetophenone, then decomposition of this intermediate by treatment
Cranwell, Philippa B.+1 more
core +1 more source
We herein report the identification of UR‐NR435 (25), a SCH‐23390‐based fluorescent ligand bearing a 5‐TAMRA dye, as suitable for fluorescence microscopy at the D1R. Single‐digit nanomolar binding affinity could be determined in radioligand competition binding and molecular brightness studies at D1‐like receptors.
Niklas Rosier+11 more
wiley +1 more source
Inhibition of 6-hydroxydopamine-induced oxidative damage by 4,5-dihydro-3H-2-benzazepine N-oxides [PDF]
A number of new analogs of 3,3-dimethyl-4,5-dihydro-3H-2-benzazepine 2-oxide, structurally related to the nitrone spin trap α-phenyl-N-tert-butylnitrone (PBN), were synthesized and evaluated for their activity in vitro as protectants against oxidative ...
Altomare, Cosimo+7 more
core +1 more source
Enantioselective palladium(0)-catalyzed C-H arylation strategy for chiral heterocycles [PDF]
Transition-metal-catalyzed C-H functionalizations have emerged as complementary and powerful tools to access molecular complexity from widely available starting materials.
Cramer, Nicolai, Saget, Tanguy
core
Reactions of [2-(Bromomethyl)phenyl](4-chlorophenyl)methanone: A New Synthesis of [1,3]Thiazolo[3,2-b][2,4]benzodiazepine, Benzimidazo[1,2-b][2,4]benzodiazepine and Benzimidazo[1,2-b][2]benzazepine Derivatives [PDF]
A new approach to the development of a number of azolo-condensed azepines and diazepines has been proposed. The method for the synthesis of [1,3]thiazolo[3,2-b][2,4]benzodiazepine, benzimidazo[1,2-b][2,4]benzodiazepineandbenzimidazo[1,2-b][2 ...
Davydov, Valentyn+2 more
core +2 more sources
In vitro activity against Leishmania and human skin permeation of miltefosine ultradeformable liposomes [PDF]
Introducción: los liposomas ultradeformables de miltefosina (LUD-MIL) constituyen una opción para el tratamiento tópico en leishmaniasis cutánea penetrando los estratos de la piel hasta la dermis, sitio donde habita el parásito.
Escobar Rivero, Patricia+2 more
core +1 more source
Preparation of substituted tetrahydro-1-benzazepines by lithiation-trapping [PDF]
The tetrahydro‐1‐benzazepine or benzo[b]azepine ring system is found in a number of drug molecules although methods to access 2,2‐disubstituted derivatives are rare. Here we report the preparation of N‐tert‐butoxycarbonyl‐2‐phenyltetrahydro‐1‐benzazepine
Aeyad+38 more
core +1 more source
Arylbenzazepines Are Potent Modulators for the Delayed Rectifier K+ Channel: A Potential Mechanism for Their Neuroprotective Effects [PDF]
(±) SKF83959, like many other arylbenzazepines, elicits powerful neuroprotection in vitro and in vivo. The neuroprotective action of the compound was found to partially depend on its D1-like dopamine receptor agonistic activity. The precise mechanism for
Bernhard, Eric J.+7 more
core +1 more source
Azabicyclo chemistry II. Synthesis of 1,5‐methano‐2,3,4,5‐tetrahydro‐1H‐2‐benzazepines. B‐norbenzomorphans [PDF]
Michael Mokotoff, Arthur E. Jacobson
openalex +1 more source
Synthesis of Sultams from Vinyl Aziridines and 1,4-Diazabicyclo[2.2.2]octane bis(sulfur dioxide) [PDF]
Sultams are an important functional group found in medicinal compounds with anticancer and enzyme inhibition activity. Traditional methods for sultam synthesis often require harsh conditions and have limited substrate scope.
Gandara, John
core +1 more source