Scalable 9-Step Synthesis of the Splicing Modulator NVS-SM2.

Date publication

mars 2018

Journal

The Journal of organic chemistry

Auteurs

Membres identifiés du Cancéropôle Est :
Dr DESAUBRY Laurent

Tous les auteurs :
Abou-Hamdan H, Désaubry L

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/29417806

Résumé

NVS-SM2, the first activator of pre-mRNA splicing, displays remarkable pharmacological in vivo activities in models of spinal muscular atrophy. Herein we describe an improved approach to the synthesis of this compound, which features a convenient introduction of sterically encumbered amine moiety onto a fluoropyridazine intermediate.

Mots clés

Benzene, chemical synthesis, Chemistry Techniques, Synthetic, Piperidines, chemical synthesis, Pyrazoles, chemical synthesis, Pyridazines, chemical synthesis, RNA Splicing, drug effects

Référence

J. Org. Chem.. 2018 Mar 2;83(5):2954-2958