Methylamine → HCID 57515840, compound

Participants

Reaction Conditions

Reaction Steps

To a flame-dried microwave vial under Ar gas was added N-((1S)-1-((1R)-2-(((4′S)-8′-chloro-6′-(2,2-dimethylpropyl)-3′,4′-dihydrospiro[cyclobutane-1,2′-pyrano[2,3-c]pyridin]-4′-yl)amino)-1-hydroxyethyl)-3-buten-1-yl)acetamide (120 mg, 267 μmol), Pd2dba3 (49 mg, 53 μmol), and DavePhos (46 mg, 117 μmol). The vial was purged with N2 5×, then THF (3 mL), methanamine (533 μl, 1067 μmol), and LiHMDS (2400 μl, 2400 μmol) were added. The vial was sealed and heated in a microwave at 110° C. for 10 min. The reaction mixture was directly purified by reverse phase HPLC to give the title compound as an amorphous white solid. MS m/z: 445.3 (M+1).

Provenance & Evidence