4-Aminotetrahydropyran → HCID 59568440, compound

HRID 1695507Notes

Reaction equation

[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2[C:12]([CH2:13][NH:14][C:15]3[CH:19]=[C:18]([C:20]([OH:22])=O)[N:17]([CH3:23])[N:16]=3)=[C:11]([CH3:24])[O:10][N:9]=2)=[N:6][CH:7]=1.[NH2:25][CH:26]1[CH2:31][CH2:30][O:29][CH2:28][CH2:27]1>>[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2[C:12]([CH2:13][NH:14][C:15]3[CH:19]=[C:18]([C:20]([NH:25][CH:26]4[CH2:31][CH2:30][O:29][CH2:28][CH2:27]4)=[O:22])[N:17]([CH3:23])[N:16]=3)=[C:11]([CH3:24])[O:10][N:9]=2)=[N:6][CH:7]=1

Participants

Reactant 2

HCID 4192234-Aminotetrahydropyran

HCID 66646190HCID 66646190, compound

Product 1

HCID 59568440HCID 59568440, compoundYield 80%

Procedure

As described for example 163c, 3-((3-(5-fluoropyridin-2-yl)-5-methylisoxazol-4-yl)methylamino)-1-methyl-1H-pyrazole-5-carboxylic acid (76 mg, 0.23 mol) was converted, using 4-aminotetrahydropyran instead of isopropylamine, to the title compound (95 mg, 80%) which was obtained as a white solid. MS: m/e=415.2 [M+H]+.

Sources & evidence

ORD record: ord-a04ca6b05d2d480783cfb813fa6ce2ce
Source dataset: uspto-grants-2012_04
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US08163728B2

Reaction notes

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