4-(6-fluoropyridin-3-yl)-1H-pyrrol-2(5H)-one → 4-(6-Fluoropyridin-3-yl)pyrrolidin-2-one
Reaction equation
[F:1][C:2]1[N:7]=[CH:6][C:5]([C:8]2[CH2:12][NH:11][C:10](=[O:13])[CH:9]=2)=[CH:4][CH:3]=1>CO.[Pd]>[F:1][C:2]1[N:7]=[CH:6][C:5]([CH:8]2[CH2:12][NH:11][C:10](=[O:13])[CH2:9]2)=[CH:4][CH:3]=1Participants
4
Reactant 1
Product 1
Reagents, catalysts & solvents 2
Procedure
To 4-(6-fluoropyridin-3-yl)-1H-pyrrol-2(5H)-one(190 mg, 1.066 mmol) in MeOH (10 mL) under N2 atmosphere was added Pd—C (227 mg, 0.213 mmol). The reaction mixture was stirred under H2 balloon at room temperature for overnight. Reaction mixture was filtered through Celite, washed with MeOH. Filtrate was evaporated. Azeotrope with toluene (x=3). Yield was 80%. Proceed for next step. LCMS (m/z): 181.0 (MH+), 0.341 min.
Workup
- customReaction mixture
- filtrationwas filtered through Celite
- washwashed with MeOH
- customFiltrate was evaporated
- custom181.0 (MH+), 0.341 min.
Sources & evidence
- ORD record
- ord-9229717d83af421c9cbec786ffe28491
- Source dataset
- uspto-grants-2016_01
- Patent number
- US09242996B2
Reaction notes
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