4-Aminotetrahydropyran → HCID 42629332, compound

HRID 83269Notes

Reaction equation

HRID 83269 reaction equation
CO[C:3](=[O:28])[C:4]1[CH:9]=[CH:8][C:7]([O:10][CH2:11][C:12]2[C:13]([C:21]3[CH:26]=[CH:25][C:24]([F:27])=[CH:23][CH:22]=3)=[N:14][O:15][C:16]=2[C:17]([F:20])([F:19])[F:18])=[N:6][CH:5]=1.[NH2:29][CH:30]1[CH2:35][CH2:34][O:33][CH2:32][CH2:31]1>>[F:27][C:24]1[CH:25]=[CH:26][C:21]([C:13]2[C:12]([CH2:11][O:10][C:7]3[CH:8]=[CH:9][C:4]([C:3]([NH:29][CH:30]4[CH2:35][CH2:34][O:33][CH2:32][CH2:31]4)=[O:28])=[CH:5][N:6]=3)=[C:16]([C:17]([F:19])([F:20])[F:18])[O:15][N:14]=2)=[CH:22][CH:23]=1

Participants

3

Procedure

As described for example 137, 6-[3-(4-fluoro-phenyl)-5-trifluoromethyl-isoxazol-4-ylmethoxy]-nicotinic acid methyl ester (100 mg, 0.25 mmol) was converted, using 4-aminotetrahydropyran instead of methylamine (2 M in THF), to the title compound (94 mg, 80%) which was obtained as a white solid. MS: m/e=466.0 [M+H]+.

Sources & evidence

ORD record
ord-2512d96635dd4437b911bee6746ff54c
Source dataset
uspto-grants-2014_09
Patent number
US08846719B2

Reaction notes

Loading…