Scalable 9-Step Synthesis of the Splicing Modulator NVS-SM2 | Zendy

Hussein AbouHamdan | Zendy; Laurent Désaubry | Zendy

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

Author(s) -

Hussein AbouHamdan,

Laurent Désaubry

Publication year - 2018

Publication title -

the journal of organic chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.2

H-Index - 228

eISSN - 1520-6904

pISSN - 0022-3263

DOI - 10.1021/acs.joc.7b03009

Subject(s) - chemistry , moiety , steric effects , rna splicing , amine gas treating , in vivo , scalability , activator (genetics) , combinatorial chemistry , biochemistry , stereochemistry , gene , organic chemistry , computer science , genetics , rna , biology , database

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.

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