849674-11-9Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS FOR MODULATING NR2F6
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Paragraph 00385, (2021/09/04)
The present disclosure relates to compounds capable of modulating the activity of NR2F6. The compounds of the disclosure may be used in methods for the prevention and/or the treatment of diseases and disorders associated with modulating NR2F6 activity.
Highly enantioselective organocatalytic oxidative kinetic resolution of secondary alcohols using chiral alkoxyamines as precatalysts: Catalyst structure, active species, and substrate scope
Murakami, Keiichi,Sasano, Yusuke,Tomizawa, Masaki,Shibuya, Masatoshi,Kwon, Eunsang,Iwabuchi, Yoshiharu
, p. 17591 - 17600 (2015/02/19)
The development and characterization of enantioselective organocatalytic oxidative kinetic resolution (OKR) of racemic secondary alcohols using chiral alkoxyamines as precatalysts are described. A number of chiral alkoxyamines have been synthesized, and their structure-enantioselectivity correlation study in OKR has led us to identify a promising precatalyst, namely, 7-benzyl-3-n-butyl-4-oxa-5-azahomoadamantane, which affords various chiral aliphatic secondary alcohols (ee up to >99%, krel up to 296). In a mechanistic study, chlorine-containing oxoammonium species were identified as the active species generated in situ from the alkoxyamine precatalyst, and it was revealed that the chlorine atom is crucial for high reactivity and enantioselectivity. The present OKR is the first successful example applicable to various unactivated aliphatic secondary alcohols, including heterocyclic alcohols with high enantioselectivity, the synthetic application of which is demonstrated by the synthesis of a bioactive compound.
PYRROL-1 -YL BENZOIC ACID DERIVATES USEFUL AS MYC INHIBITORS
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Paragraph 00358, (2014/05/24)
The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The p
Enzyme-catalyzed kinetic resolution of N-Boc-trans-3-hydroxy-4- phenylpyrrolidine
Faigl, Ferenc,Kovacs, Ervin,Balogh, Dora,Holczbauer, Tamas,Czugler, Matyas,Simandi, Bela
, p. 25 - 32 (2014/01/06)
The first enzyme-catalyzed kinetic resolution of tert-butyl-3-hydroxy-4- phenylpyrrolidine-1-carboxylate is presented. Enzyme, solvent and temperature optimization resulted in a new resolution method with E = 40 enantioselectivity. The acetate derivative of the (+)-(3S,4R) enantiomer formed while the (-)-(3R,4S) isomer remained intact. Very good enantioselectivities (E > 200) were achieved in the enzyme-catalyzed alcoholysis of the racemic acetate in i-propanol and t-butanol where the (+)-(3S,4R) enantiomer was prepared in pure form (ee > 99.7%). Absolute configuration of the (-)-(3R,4S)-enantiomer was determined by single crystal X-ray diffraction method. [Figure not available: see fulltext.]
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine
Lin, Peter,Chang, Lehua,DeVita, Robert J.,Young, Jonathan R.,Eid, Ronsar,Tong, Xinchun,Zheng, Song,Ball, Richard G.,Tsou, Nancy N.,Chicchi, Gary G.,Kurtz, Marc M.,Tsao, Kwei-Lan C.,Wheeldon, Alan,Carlson, Emma J.,Eng, WaiSi,Burns, H. Donald,Hargreaves, Richard J.,Mills, Sander G.
, p. 5191 - 5198 (2008/03/13)
SAR studies on amides, ureas, and vinylogous amides derived from pyrrolidine led to the discovery of several potent hNK1 antagonists. One particular vinylogous amide (45b) had excellent potency, selectivity, pharmacokinetic profile, and functio
PHENYL PYRROLIDINE ETHER TACHYKININ RECEPTOR ANTAGONISTS
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, (2008/06/13)
The present invention is directed to certain phenyl pyrrolidine ether compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical f
