Über Dibenzo‐thiazepin‐Derivate und ihre pharmakologische Wirkung

Abstract

Im Rahmen unserer Arbeiten uber basisch substituierte Derivate von N-und S-Atome enthaltenden heterocyclischen Verbindungen haben wir uns seit langerer Zeit mit der Darstellung von Abkommlingen des Dibenzo-thiazepins 2, befasst.Die folgenden Ausfuhrungen teilen wir in drei Abschnitte: der erste und der zweite handeln von der Darstellung von Derivaten der Dibenzo-thiazepin-11-one bzw. der Dibenzo-thiazepine, wahrend im dritten die pharmakologischen Haupteigenschaften dieser Verbindungen besprochen werden.

2-(2-Pyridyl)-1,2-diarylalkanols as Hypocholesteremic Agents

“…;02: C, 77.18; H, 7.97; K, 6 work-up were similar to that described above for 16 and 17. Calcd for C26H32?…”

“…Caled for (%,1 li3X(): (', 83.49: H,5.53. Found: (',83.31: H,5.75,l,2,3,3,6,-lnaphthol.-A solution of 4.7 g (0.05 mole) of 2-pi coline in 50 ml of ether was slowly added at 0°to an ether solution (250 ml) of phenyllithium from 0.7 g (0.1 g-atom) of lithium wire and 7.9 g (0.0.5 mole) of bromobenzene. The solution was then stirred for 1 hr at 0°.…”

Synthesis of 5-oxo-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-carboxylic acids corresponding nitriles, and related bridged lactones, hemiketals, lactams, amines, amidoximines, and amidines (5,10-epoxymethano and 5,10-iminomethano compounds)

“…Caled for C16H17N-HC1: C, 73.97; H, 6.98; N, 5.39. Found: C, 74.30; H, 6.92; N, 5.39. 13-Hydroxy-10,l l-dihydro-5,10-iminomethano-5H-dibenzo-[a,d]cyclohepten-12-one (22).-Hydroxy]amine HC1 (35 g) in water (20 ml) was neutralized at 0°b y slowly adding NaOH (14 g) in water (10 ml), ethylene glycol (120 ml) was added, the solution was filtered, lactone 13a (5.25 g) was added; the solution was refluxed 13 hr and kept at 100°for 4 days. The product, crystallized on addition of water, was collected, washed with water and ether, and dried: yield 3.75 g; mp 233-2360, raised on recrystallization from ether to mp 237-239°; ir 6.05 µ and bonded OH; nmr (DMSO) 5.41 (s, 1, benzhydryl proton).…”

Microwave‐Assisted Synthesis of Substituted Dibenzo[b,f][1,4]thiazepines, Dibenzo[b,f][1,4]oxazepines, Benzothiazoles, and Benzimidazoles

“…1,4‐Dibenzothiazepine has been synthesized by reaction of lithiated 2‐aminodiphenyl sulfide with DMF . Cyclization of o ‐nitrobenzene halides with o ‐thiosalicylic acid esters, followed by reduction and dehydration, also afford dibenzothiazepine products . We describe herein a novel and efficient synthesis of dibenzo[ b , f ][1,4]thiazepines and of the related heteroaromatic derivatives in one‐pot procedure.…”