139040-41-8Relevant academic research and scientific papers
Application of piperazine structure containing compound to preparation of LSD1 (Lysine Specific Demethylase 1) inhibitor
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Paragraph 0017, (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.
Synthesis of 1- and 4-substituted piperazin-2-ones via Jocic-type reactions with N-substituted diamines
Perryman, Michael S.,Earl, Matthew W. M.,Greatorex, Sam,Clarkson, Guy J.,Fox, David J.
supporting information, p. 2360 - 2365 (2015/03/04)
Enantiomerically-enriched trichloromethyl-containing alcohols, obtained by asymmetric reduction, can be transformed regioselectively into 1-substituted piperazinones by modified Jocic reactions with little or no loss of stereochemical integrity. This meth
Trichloromethyl ketones: Asymmetric transfer hydrogenation and subsequent Jocic-type reactions with amines
Perryman, Michael S.,Harris, Matthew E.,Foster, Jade L.,Joshi, Anushka,Clarkson, Guy J.,Fox, David J.
supporting information, p. 10022 - 10024 (2013/10/22)
Amino-amides are important pharmaceutical building-blocks. The enantioselective reduction of trichloromethyl ketones using ruthenium transfer hydrogenation catalysts is reported. The products react in a range of Jocic-type reactions to give enantiomerically enriched amino-amides.
Meerwein-Ponndorf-Verley alkynylation of aldehydes: Essential modification of aluminium alkoxides for rate acceleration and asymmetric synthesis
Ooi, Takashi,Miura, Tomoya,Ohmatsu, Kohsuke,Saito, Akira,Maruoka, Keiji
, p. 3312 - 3319 (2007/10/03)
A novel carbonyl alkynylation has been accomplished based on utilization of the Meerwein-Ponndorf-Verley (MPV) reaction system. The success of the MPV alkynylation crucially depends on the discovery of the remarkable ligand acceleration effect of 2,2′-biphenol. For example, the alkynylation of chloral (2c) with the aluminium alkoxide 6 (R = Ph), prepared in situ from Me3Al, 2,2′-biphenol and 2-methyl-4-phenyl-3-butyn-2-ol (1a) as an alkynyl source, proceeded smoothly in CH2Cl2 at room temperature to give the desired propargyl alcohol 3ca in almost quantitative yield after 5 h stirring. The characteristic feature of this new transformation involving no metal alkynides can be visualized by the fact that the alkynyl group bearing keto carbonyl was transferred successfully to aldehyde carbonyl without any side reactions on keto carbonyl. Although the use of (S)-1,1′-bi-2-naphthol and its simple analogues was found to be unsuitable for inducing asymmetry in this reaction, design of new chiral biphenols bearing a certain flexibility of the biphenyl axis led to satisfactory results in terms of enantioselectivity as well as reactivity.
A CATALYTIC ENANTIOSELECTIVE SYNTHESIS OF CHIRAL MONOSUBSTITUTED OXIRANES
Corey, E. J.,Helal, Christopher J.
, p. 5227 - 5230 (2007/10/02)
A new catalytic enentioselective synthesis of monosubstituted oxiranes has been developed from achiral trichloromethyl ketones by (a) enentioselective carbonyl reduction, (b) selective bis-dechlorination and (c) base-induced ring closure of the resulting chlorohydrins.
A new process for the generation of 1,3,2-oxazaborolidines, catalysts for enantioselective synthesis
Corey,Link
, p. 4141 - 4144 (2007/10/02)
A simple and easily reproducible procedure for the formation of 1,3,2-oxazaborolidines from β-amino alcohols and bis(trifluoroethyl) alkylboronates, is reported along with a new synthesis of the latter.
A new process for the enantioselective synthesis of chiral α-aryloxy- and α-hydroxy acids
Corey,Link, John O.
, p. 3431 - 3434 (2007/10/02)
Chiral trichloromethyl carbinols 3, readily available by catalytic enantioselective reduction of trichloromethyl ketones, are converted with inversion of configuration into chiral α-aryloxy and α-hydroxy carboxylic acid derivatives.
