pf 07258669  (MedChemExpress)

Journal: Communications Chemistry

Article Title: Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines

doi: 10.1038/s42004-023-01012-2

Figure Lengend Snippet: a Prior art: Pfizer’s enantioselective synthesis of core ( 35 ) of melanocortin MC4 receptor antagonist 5 . b Our (racemic) synthesis of core ( 35 ) of melanocortin MC4 receptor antagonist 5 .

Article Snippet: Finally, we sought to apply our methodology to a concise synthesis of the spirocyclic THN core ( 35 ) of Pfizer’s MC4R antagonist PF-07258669 5 , which was previously synthesised in 15 total steps (11 steps LLS) (Fig. ) .

Techniques:

Journal: Communications Chemistry

Article Title: Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines

doi: 10.1038/s42004-023-01012-2

Figure Lengend Snippet: a Tetrahydronaphthyridine (THN) isomers. b THNs 1 in drug development. c Spirocyclic THNs 1 in drug development.

Article Snippet: The simplifying power of the methodology is illustrated by a concise synthesis of the spirocyclic THN core ( 35 ) of Pfizer’s MC4R antagonist PF-07258669 ( 5 ).

Techniques:

Journal: Communications Chemistry

Article Title: Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines

doi: 10.1038/s42004-023-01012-2

Figure Lengend Snippet: a Selected synthetic routes to (spirocyclic) 1,8-THNs. b This work.

Article Snippet: The simplifying power of the methodology is illustrated by a concise synthesis of the spirocyclic THN core ( 35 ) of Pfizer’s MC4R antagonist PF-07258669 ( 5 ).

Techniques: