Arylethylamines represent a privileged scaffold in pharmaceutical compounds and form the backbone of many medical drugs, including those used for treating neurological diseases and pain. Their biomedical significance has inspired new synthetic methods that rely on transition metal-catalyzed aminoarylation reaction to an alkene, often in conjunction with a photoredox catalyst or a photosensitizer, and guided by a directing or stabilizing group. Here, we introduce a simple and effective method for azidoarylation of unactivated alkenes under transition metal-free conditions. Visible or near-UV light irradiation of readily available triarylbismuth dichlorides generates an aryl radical that selectively adds to the alkene, and the resulting homobenzyl radical is intercepted by an amine equivalent. This method offers a broad substrate scope and also enables aryl chlorination and arylcyanation of unactivated alkenes.

2012-01-01·Organic & biomolecular chemistry3区 · 化学

Synthesis of (S)-(+)-cericlamine through lipase-catalyzed aminolysis of azo acetates

3区 · 化学

Article

作者: Agnes Prechter ; Markus R. Heinrich ; Harald Gröger

The kinetic enzymatic resolution of azo acetates via aminolysis with Candida antarctica lipase B has been investigated using benzylamine as amine component. The products obtained from this biotransformation in high enantiomeric purity can serve as valuable precursors for various amino alcohols, as exemplified by the synthesis of the serotonin reuptake inhibitor (S)-(+)-cericlamine.

1996-11-01·Biological psychiatry1区 · 医学

Reduced inhibitory potency of serotonin reuptake blockers on central serotoninergic neurons in rats selectively deprived of rapid eye movement sleep

1区 · 医学

Article

作者: Thierry Jolas ; Michel Hamon ; Michel Chastanet ; Corinne Maudhuit ; Joëlle Adrien

Previous studies showed that chronic deprivation of rapid eye movement (REM) sleep had the same behavioral effects as antidepressant drugs in helpless rats. Since long-term treatment with antidepressants is known to affect central serotoninergic neurotransmission, we investigated whether REM sleep deprivation also exerts an influence on the activity of serotoninergic neurons within the dorsal raphe nucleus (DRN) in rats. REM sleep deprivation was performed using the platform technique. Recording of serotoninergic neurons in the DRN revealed no difference in the basal firing rate, but a reduced inhibitory response to the selective serotonin (5-HT) reuptake blockers cericlamine and citalopram after repeated but not acute REM sleep deprivation. These observations suggest that REM sleep deprivation renders serotoninergic DRN neurons less sensitive to the inhibitory effect of 5-HT reuptake blockers, probably because of functional desensitization of somatodendritic 5-HT1A autoreceptors, like that previously reported after chronic treatment with several antidepressants. Accordingly, REM sleep deprivation might alleviate depression through neurophysiological mechanisms similar to those induced by antidepressants.

100 项与 Cericlamine hydrochloride 相关的药物交易

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