L-Alaninol → 3-((3S,4S)-3-Fluoro-tetrahydro-pyran-4-ylamino)-isoquinoline-6-carboxylic acid [(S)-1-(3-chloro-4-fluoro-phenyl)-2-hydroxy-ethyl]-amide

Participants

Reaction Steps

3-((3S,4S)-3-Fluoro-tetrahydro-pyran-4-ylamino)-isoquinoline-6-carboxylic acid [(S)-1-(3-chloro-4-fluoro-phenyl)-2-hydroxy-ethyl]-amide (II-53) was prepared analogously except in step 2, (S)-2-aminopropan-1-ol was replaced with (3S,4S)-3-fluorotetrahydro-2H-pyran-4-amine (71c) and in step 5, 50c was replaced with (S)-2-amino-2-(3-chloro-4-fluoro-phenyl)ethanol hydrochloride (62f). 1H NMR (500 MHz, MeOH-d4): δ 8.90 (s, 1H), 8.08 (s, 1H), 7.90 (d, J=8.5 Hz, 1H), 7.60-7.57 (m, 2H), 7.43-7.30 (m, 1H), 7.27-7.23 (m, 1H), 6.93 (s, 1H), 5.21-5.18 (m, 1H), 4.86-4.73 (m, 1H), 4.27-4.12 (m, 2H), 4.05-4.02 (m, 1H), 3.91-3.86 (m, 2H), 3.75-3.62 (m, 2H), 2.04-1.96 (m, 1H), 1.90-1.87 (m, 1H),

Provenance & Evidence