912277-45-3Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR INHIBITING HISTONE DEMETHYLASES
-
Paragraph 00668, (2016/03/22)
The present application relates to compounds being of Formula (I), (II), (III), (IV), (V), (VI), (Ilia), (Illb), (IIIc), (Hid), (Hie), (Illf), and (Illg). Compounds of Formula (I) have the structure: wherein Q, R1, R18, R19, M, A and Y are as defined herein. The compounds of the application can modulate the activity of histone demethylases (HDMEs), and can be useful for the prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, e.g., cancer.
Enantiopure synthesis of 7-(1-pyrindanyl)propargyl ethers as rasagiline analogues via chemical or enzymatic resolution of 1-pyrindan-7-ol
Sousa, Carlos A. D.,Sampaio-Dias, Ivo E.,Rizzo-Aguiar, Fabio,Garcia-Mera, Xerardo,Rodríguez-Borges, José E.
, p. 104509 - 104515 (2015/12/24)
In this work, the enantiopure synthesis of 7-(1-pyrindanyl)propargyl ethers - rasagiline analogues - via chemical and/or enzymatic resolution of the racemic precursor 1-pyrindan-7-ol is described. (R)-Methoxyphenylacetic acid - (R)-MPAA - and (S)-methoxyphenylacetic acid - (S)-MPAA were used as chemical resolution agents, whereas Candida antarctica lipase B (CALB) was employed as kinetic resolution catalyst. The enzymatic resolution was successfully achieved by two different approaches: (1) transesterification of racemic 1-pyrindan-7-ol, which was found to selectively acylate the (R)-enantiomer with high efficiency; (2) hydrolysis of the racemic 7-(1-pyrindanyl)acetate, which was also highly selective to the (R)-enantiomer. The enzymatic hydrolysis was performed in a non-aqueous solvent using a lipase with significant absorbed water content. The configuration of the two enantiomers of 1-pyrindan-7-ol (and consequently of the 7-(1-pyrindanyl)propargyl ethers) were unequivocally determined by X-ray crystallography and/or specific optical rotation.
Iridium catalysts with bicyclic pyridine-phosphinite ligands: Asymmetric hydrogenation of olefins and furan derivatives
Kaiser, Stefan,Smidt, Sebastian P.,Pfaltz, Andreas
, p. 5194 - 5197 (2007/10/03)
(Chemical Equation Presented) Superior bicyclics: Iridium catalysts as 1 derived from pyridine-phosphinite ligands considerably extend the scope of asymmetric hydrogenation. In addition to various unfunctionalized and functionalized olefins, furans, and benzofurans, for which no catalysts were known before, are also hydrogenated with high enantioselectivity (see scheme).
