5650-45-3Relevant articles and documents
Enantioselective and Diastereoselective Construction of Chiral Amino Alcohols by Iridium-f-Amphox-Catalyzed Asymmetric Hydrogenation via Dynamic Kinetic Resolution
Wu, Weilong,You, Cai,Yin, Congcong,Liu, Yuanhua,Dong, Xiu-Qin,Zhang, Xumu
, p. 2548 - 2551 (2017/05/24)
The iridium-f-amphox-catalyzed asymmetric hydrogenation of racemic α-amino β-unfunctionalized ketones proceeds via a DKR (dynamic kinetic resolution) process for the construction of various chiral N,N-disubstituted α-amino β-unfunctionalized alcohols in quantitative yields with excellent enantioselectivities and diastereoselectivities (all products >99% ee and >99:1 dr, TON up to 100 000). Importantly, this catalytic asymmetric hydrogenation with a DKR process provided a highly efficient and powerful synthetic strategy for the preparation of key chiral intermediates of the preclinical antitumor agent (S,S)-R116010.
N-Bromosuccinimide promoted and base switchable one pot synthesis of α-imido and α-amino ketones from styrenes
Shinde, Mahesh H.,Kshirsagar, Umesh A.
supporting information, p. 858 - 861 (2016/01/15)
An N-Bromosuccinimide (NBS) promoted one pot strategy for the synthesis of α-amino functionalized aryl ketones starting from commercially available styrenes has been developed. NBS participates in multiple tasks, such as bromonium ion formation, oxidation of bromohydrin and providing a nucleophilic nitrogen source. The reaction can easily be switched between α-imido and α-amino ketones by the choice of base. This one pot strategy was successfully applied for the synthesis of psychoactive drug candidates, amfepramone, mephedrone and 4-MEC.
Copper bromide reagent and its preparation method, α--aminobenzene acetone and its process for synthesis of derivatives of
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Paragraph 0025; 0026, (2017/02/28)
The invention discloses a copper bromide reagent, a preparation method thereof, and a synthesis method of alpha-amido propiophenone and derivative thereof. Copper bromide cheap in industry and 2,6-bi[4-(1,1-dimethyl)-2-oxazoline-2-base] pyridine react to directly obtain high yield of high-purity copper bromide reagent, in addition, the copper bromide reagent and propiophenone containing multiple important functional groups have good reaction activity. Due to the characteristic, high yield of alpha-amido propiophenone and derivative thereof can be obtained in mild conditions, conventional expensive azoic compound materials are not used, the cost is lowered to a large extent, the operation requirement is also lowered, and alpha-amido propiophenone and derivative thereof have good application prospect in industry.