138647-51-5Relevant articles and documents
A versatile synthesis of 4-aryl tetrahydropyridines via palladium mediated Suzuki cross-coupling with cyclic vinyl boronates
Eastwood, Paul R.
, p. 3705 - 3708 (2000)
A simple preparation of cyclic vinyl boronates derived from the vinyl triflates of N-protected tetrahydropyridines is described. Suzuki coupling of the boronates with aryl bromides, iodides and triflates proceeds in good yield to give 4-aryl tetrahydropyridines. (C) 2000 Elsevier Science Ltd.
20-HETE FORMATION INHIBITORS
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Paragraph 0257-0260, (2020/08/23)
This disclosure provides novel heterocyclic compounds and methods for inhibiting the enzyme CYP4. Further disclosed methods include: a method of inhibiting the biosynthesis of 20-hydroxyeicosatetraenoic acid (20-HETE) in a subject in need thereof and a method of producing neuroprotection and decreased brain damage by preventing cerebral microvascular blood flow impairment and anti-oxidant mechanisms in a subject experiencing or having experienced an ischemic event.
Catalytic Friedel-Crafts Reactions on Saturated Heterocycles and Small Rings for sp3-sp2 Coupling of Medicinally Relevant Fragments
Croft, Rosemary A.,Dubois, Maryne A. J.,Boddy, Alexander J.,Denis, Camille,Lazaridou, Anna,Voisin-Chiret, Anne Sophie,Bureau, Ronan,Choi, Chulho,Mousseau, James J.,Bull, James A.
supporting information, p. 5385 - 5395 (2019/06/24)
gem-Diarylheterocycles display a wide range of biological activity. Here we present a systematic study into the formation of 4- to 6-membered O- and N-heterocycles and cyclobutanes bearing the diaryl motif through a catalytic Friedel–Crafts reaction from the corresponding benzylic alcohols. 3,3-Diaryltetrahydrofurans, 4,4-diaryltetrahydropyrans, 3,3-diarylpyrrolidines, 4,4-diaryl-piperidines, as well as diarylcyclobutanes are examined, with results for 3,3-diaryloxetanes and 3,3-diarylazetidines presented for comparison. Three catalytic systems are investigated for each substrate [Ca(II), Li(I) and Fe(III)], across preinstalled aromatic groups of differing electronic character. In most cases examined, the diaryl product is obtained directly from the alcohol with good yields using the most appropriate catalyst system. In the absence of a nucleophile, the olefins from the 5- and 6-membered substrates by elimination of water are obtained under the same reaction conditions.