90685-59-9Relevant articles and documents
SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE
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Page/Page column 169, (2020/12/11)
The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.
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.
Synthesis of New Propargylated 1-Pyrindane Derivatives as Rasagiline Analogues
Pereira, Cidáliasilva,Salgado, Sofia,Rizzo-Aguiar, Fabio,Garcia-Mera, Xerardo,Rodríguez-Borges, Josée.
supporting information, p. 837 - 838 (2013/05/21)
Rasagiline is a compound with important neuroprotective activity applicable to the treatment of neurodegenerative diseases. This work describes an easy and straightforward methodology to the synthesis of new propargylated rasagiline analogues derived from commercially available 6,7-dihydro-5H-cyclopenta[b] pyridine. Georg Thieme Verlag Stuttgart - New York.