131981-95-8Relevant academic research and scientific papers
The synthesis of new diastereomers of (4S,8aS)- and (4R,8aS)-4-phenyl-perhydropyrrole[1,2-a]pyrazine-1,3-dione
Herold, Franciszek,Dawidowski, Maciej,Wolska, Irena,Chodkowski, Andrzej,Kleps, Jerzy,Turlo, Jadwiga,Zimniak, Andrzej
, p. 2091 - 2098 (2007)
The synthesis of new (4S,8aS)- and (4R,8aS)-4-phenyl-perhydropyrrole[1,2-a]pyrazine-1,3-diones in the cyclocondensation reaction of the respective derivatives of l-prolineamide is described. The effect of the amount of NaOEt, temperature, and reaction time on the proportions of diastereomers formed in the cyclocondensation reaction was examined. The structures of the diastereomers were confirmed by GC/MS, HRMS, HPLC, XRD, and 1H and 13C NMR investigations.
Application of piperazine structure containing compound to preparation of LSD1 (Lysine Specific Demethylase 1) inhibitor
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Paragraph 0019, (2017/09/29)
The invention discloses application of a piperazine structure containing compound to the preparation of a histone lysine specific demethylase (LSD1) inhibitor. The structural general formula of the compound is as shown in the following descriptions (wherein, A is hydrogen, carbonyl or thiocarbonyl) or a configurational isomer and a pharmaceutical salt thereof, or is as shown in the following descriptions or a pharmaceutical salt thereof. The compound has an obvious inhibition effect on the LSD1, can be prepared into the LSD1 inhibitor, and is used for preventing and treating a disease related to the activity of the histone LSD1.
Either diastereofacial differentiation in the reaction of chiral thiomethylketones with appropriate organometallics
Fujisawa,Takemura,Ukaji
, p. 5479 - 5482 (2007/10/02)
Introduction of sulfur atom instead of oxygen into α-position to ketone was found to be crucial for efficient diastereofacial differentiation; i.e., either diastereomer of tertiary alcohol could be obtained by the reaction of organometallics to chiral thiomethylketones derived from (S)-2-mercapto-2-phenylethanol and α-halo ketones. For example, MeLi attacked from si-face, while Me2Zn preferred re-facial attack. In addition, both enantiomers of 1,2-O-isopropylidene-2-methyl-1,2,5-pentanetriol, a key intermediate for the synthesis of frontalin, were successfully synthesized utilizing the present method.
