20099-96-1Relevant academic research and scientific papers
Solvent-Free Synthesis of α-Amino Ketones from α-Hydroxyl Ketones via A Novel Tandem Reaction Sequence Based on Heyns Rearrangement
Li, Ling-Yu,Zeng, Qing-Le,Li, Guang-Xun,Tang, Zhuo
supporting information, p. 694 - 699 (2019/03/26)
Heyns rearrangement have been famous for carbohydrate chemists for several decades. However, this reaction was underrated as a useful method for synthetic chemists due to preparative shortcomings. Herein we developed an efficient method for the synthesis of pharmaceutically important α-amino ketones from readily available α-hydroxy ketones and secondary amines through a tandem reaction sequence based on Heyns rearrangement. The reaction smoothly proceeded by using catalytic PTSA as catalyst without solvent. Primary and secondary α-hydroxy ketones were readily used and regioselectively afforded the correspondingly α-amino ketones with moderate yield.
Coupling of methyl ketones and primary or secondary amines leading to α-ketoamides
Wei, Wei,Shao, Ying,Hu, Huayou,Zhang, Feng,Zhang, Chao,Xu, Yuan,Wan, Xiaobing
, p. 7157 - 7165 (2012/11/07)
A metal-free oxidative coupling of methyl ketones and primary or secondary amines to α-ketoamides has been developed. Four intermediates, α-iodoketone, α-aminoketone, iminium intermediate, and α-hydroxy amine have been identified through a series of control experiments. The atom-economic methodology can be scaled-up, tolerates a variety of functional groups, and is operationally simple.
MORPHOLINYL AND PYRROLIDINYL ANALOGS
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Page/Page column 67, (2008/06/13)
The present invention relates to morpholinyl, and pyrrolidinyl analogs, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
