- Cobalt-Catalyzed Markovnikov-Selective Radical Hydroacylation of Unactivated Alkenes with Acylphosphonates
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Acylphosphonates having the 5,5-dimethyl-1,3,2-dioxophosphinanyl skeleton are developed as efficient intermolecular radical acylation reagents, which enable the cobalt-catalyzed Markovnikov hydroacylation of unactivated alkenes at room temperature under mild conditions. The protocol exhibits broad substrate scope and wide functional group compatibility, providing branched ketones in satisfactory yields. A mechanism involving the Co-H mediated hydrogen atom transfer and subsequent trapping of alkyl radicals by acylphosphonates is proposed.
- Fang, Yewen,He, Jiayan,Li, Chaozhong,Li, Yi,Song, Tao,Zhang, Benxiang
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p. 4955 - 4961
(2021/05/04)
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- C-H functionalisation of aldehydes using light generated, non-stabilised diazo compounds in flow
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The difficulty in accessing and safely utilising non-stabilised diazo species has in the past limited the application of this class of compounds. Here we explore further the use of oxadiazolines, non-stabilised diazo precursors which are bench stable, in direct, non-catalytic, aldehyde C-H functionalisation reactions under UV photolysis in flow and free from additives. Commercially available aldehydes are coupled to afford unsymmetrical aryl-alkyl and alkyl-alkyl ketones while mild conditions and lack of transition metal catalysts allow for exceptional functional group tolerance. Examples are given on small scale and in a larger scale continuous production.
- Dingwall, Paul,Greb, Andreas,Crespin, Lorène N.S.,Labes, Ricardo,Musio, Biagia,Poh, Jian-Siang,Pasau, Patrick,Blakemore, David C.,Ley, Steven V.
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supporting information
p. 11685 - 11688
(2018/11/02)
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- Methods and compositions for the treatment and prevention of sexual dysfunction
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Methods are disclosed for the treatment and prevention of sexual. The methods comprise the administration of a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Pharmaceutical compositions and dosage forms are also disclosed that comprise a dopamine reuptake inhibitor and optionally an additional pharmacologically active compound. Preferred dopamine reuptake inhibitors are racemic or optically pure sibutramine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof. Preferred additional pharmacologically active compounds include drugs that affect the central nervous system, such as 5-HT3antagonists.
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- Salts of sibutramine metabolites, methods of making sibutramine metabolites and intermediates useful in the same, and methods of treating pain
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Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.
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- Methods of using sibutramine metabolites in combination with a phosphodiesterase inhibitor to treat sexual dysfunction
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Methods are disclosed for the treatment and prevention of male and female sexual function disorders which comprise a racemic or optically pure sibutramine metabolite and a phosphodiesterase inhibitor.
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- Methods of treating and preventing attention deficit disorders
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Methods are disclosed for the treatment and prevention of affective disorders with racemic or optically pure sibutramine metabolites and pharmaceutically acceptable salts, solvates, and clathrates thereof.
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