4-Aminotetrahydropyran → HCID 25132481, compound

HRID 2262548Notes

Reaction equation

CO[C:3](=[O:30])[C:4]1[CH:9]=[CH:8][C:7]([N:10]2[CH:14]=[C:13]([C:15]3[C:16]([C:24]4[CH:29]=[CH:28][CH:27]=[CH:26][CH:25]=4)=[N:17][O:18][C:19]=3[C:20]([F:23])([F:22])[F:21])[N:12]=[CH:11]2)=[N:6][CH:5]=1.[NH2:31][CH:32]1[CH2:37][CH2:36][O:35][CH2:34][CH2:33]1>>[C:24]1([C:16]2[C:15]([C:13]3[N:12]=[CH:11][N:10]([C:7]4[CH:8]=[CH:9][C:4]([C:3]([NH:31][CH:32]5[CH2:37][CH2:36][O:35][CH2:34][CH2:33]5)=[O:30])=[CH:5][N:6]=4)[CH:14]=3)=[C:19]([C:20]([F:22])([F:21])[F:23])[O:18][N:17]=2)[CH:29]=[CH:28][CH:27]=[CH:26][CH:25]=1

Participants

Reactant 2

HCID 4192234-Aminotetrahydropyran

HCID 25132124HCID 25132124, compound

Product 1

HCID 25132481HCID 25132481, compoundYield 86%

Procedure

As described for Example 18, 6-[4-(3-phenyl-5-trifluoromethyl-isoxazol-4-yl)-imidazol-1-yl]-nicotinic acid methyl ester (100 mg, 0.24 mmol), was converted, using 4-aminotetrahydropyran instead of cyclopropanemethylamine, to the title compound (110 mg, 86%) which was obtained as a white solid. MS: m/e=484.2 [M+H]+.

Sources & evidence

ORD record: ord-e127fff1a5ec4e40b6ad14ec62081f91
Source dataset: uspto-grants-2010_12
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US07851469B2

Reaction notes

Loading…