[EN] PRMT5 INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE PRMT5 ET LEURS UTILISATIONS
申请人:EPIZYME INC
公开号:WO2014100716A1
公开(公告)日:2014-06-26
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
The rational design and application of new chiral phosphonates for the enantiomeric excess determination of unprotected amino acids. Remarkable pH dependency of the diastereomeric shift differences.
作者:Ron Hulst、N.Koen de Vries、Ben L. Feringa
DOI:10.1016/s0040-4020(01)85665-9
日期:1994.1
Diastereomeric amide derivatives of chiral phosphorinane 8 and unprotectedaminoacids are easily prepared in aqueous solutions, showing well separated signals in the 31P NMR spectra allowing accurate enantiomeric excess determination. Moreover, the obtained diastereomeric shift dispersion appears to be highly pH dependent, indicating the influence of intramolecular ion pair formation on the diastereomeric
手性膦烷8的非对映体酰胺衍生物和未保护的氨基酸很容易在水溶液中制备,在31 P NMR光谱中显示出分离良好的信号,从而可以进行准确的对映体过量测定。此外,所获得的非对映异构体分散体似乎高度依赖pH,表明分子内离子对的形成对非对映异构体分散体的影响。
Asymmetric synthesis of β-dialkylamino alcohols by transfer hydrogenation of α-dialkylamino ketones
Transfer hydrogenation of representative aryl and heteroaryl dialkylaminomethyl ketones with formic acid-triethylamine, catalyzed by RuCl[(R,R)-TsDPEN](eta-p-cymene), produces the corresponding beta-dialkylamino alcohols, 97-99% ee, in 50-73% yields. Asymmetric synthesis of (R)-macromerine, 98% ee, the cactus Coryphantha macromeris alkaloid, is also described. (C) 2009 Elsevier Ltd. All rights reserved.
Yadav, Ashok K.; Manju, Meera, Indian Journal of Chemistry - Section B Organic and Medicinal Chemistry, 2006, vol. 45, # 12, p. 2770 - 2772