103-46-8Relevant articles and documents
Bivalent SIRT1 inhibitors
Wang, Juan,Zang, Wenwen,Liu, Jiajia,Zheng, Weiping
, p. 180 - 186 (2017)
In the current study, bivalent compounds 1–17 constructed by covalently linking the ?-amino group of lysine in a tripeptidic scaffold to a functionality via a linker were prepared and examined for their inhibitory potencies against SIRT1, a prototypical member of the β-nicotinamide adenine dinucleotide (β-NAD+)-dependent sirtuin family of protein Nε-acyl-lysine deacylases. A few of them were found to be stronger SIRT1 inhibitors than the N?-acetyl-lysine-containing monovalent counterparts 18 and 19. As exemplified with compounds 6 and 18, a bivalent SIRT1 inhibitor could exhibit a greater degree of inhibitory selectivity among SIRT1/2/3 than the corresponding monovalent counterpart. This study has laid a foundation for the future development of superior bivalent inhibitors against the (patho)physiologically and therapeutically important sirtuin family of deacylase enzymes.
Co-production method of thionocarbamate and benzyl thioether acetic acid and application of the method
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Paragraph 0081-0082, (2019/12/02)
The invention discloses a co-production method of thionocarbamate and benzyl thioether acetic acid and application of the method. The method comprises the following steps: with xanthate and benzyl chloride as initial raw materials, and performing esterification reaction to obtain benzyl xanthate; carrying out ammonolysis on benzyl xanthate by using primary amine to obtain thionocarbamate and benzyl mercaptan; further adding sodium chloroacetate into the mixture for reaction, thus generating benzyl thioether sodium acetate; finally, performing liquid separation to obtain the thionocarbamate collecting agent and a water phase containing benzyl thioether sodium acetate. The benzyl thioether sodium acetate-containing water phase can further react with benzyl chloride to obtain benzyl thioetherbenzyl acetate or be acidified and esterified with fatty alcohol to generate benzyl thioether alkyl acetate, and the two ester compounds can be subjected to hydroximation to synthesize benzyl thioether ethyl hydroximic acid. The method solves the problems of difficult recovery, difficult utilization and unpleasant smell of the byproduct sulfhydryl compound in the traditional thionocarbamate process, realizes co-production of benzyl thioether acetic acid and derivatives thereof, and improves the reaction efficiency.
Synthesis of Cyclic α-Diazo-β-keto Sulfoxides in Batch and Continuous Flow
McCaw, Patrick G.,Buckley, Naomi M.,Eccles, Kevin S.,Lawrence, Simon E.,Maguire, Anita R.,Collins, Stuart G.
, p. 3666 - 3679 (2017/04/11)
Diazo transfer to β-keto sulfoxides to form stable isolable α-diazo-β-keto sulfoxides has been achieved for the first time. Both monocyclic and benzofused ketone derived β-keto sulfoxides were successfully explored as substrates for diazo transfer. Use of continuous flow leads to isolation of the desired compounds in enhanced yields relative to standard batch conditions, with short reaction times, increased safety profile, and potential to scale up.
