Water → 1-(3-Fluoropyridin-2-yl)piperidin-4-one
Reaction equation
[F:1][C:2]1[C:3]([N:8]2[CH2:17][CH2:16][C:11]3(COOC3)[CH2:10][CH2:9]2)=[N:4][CH:5]=[CH:6][CH:7]=1.[OH2:18]>C(O)(=O)C>[F:1][C:2]1[C:3]([N:8]2[CH2:17][CH2:16][C:11](=[O:18])[CH2:10][CH2:9]2)=[N:4][CH:5]=[CH:6][CH:7]=1Participants
4
Reactant 2
Product 1
Reagents, catalysts & solvents 1
Procedure
8-(3-fluoro-pyridin-2-yl)-2,3-dioxa-8-azaspiro[4.5]decane 17 (347 g, 1.456 Mol) was dissolved in acetic acid (700 mL) and water (140 mL) and the mixture heated to 85° C. under nitrogen for 18 h. LC/MS shows the reaction at 92% conversion at this stage. The mixture was evaporated to dryness in vacuo, to leave orange oil. This material was used directly in the next step without further purification
Workup
- customthe reaction at 92% conversion at this stage
- customThe mixture was evaporated to dryness in vacuo
- customto leave orange oil
- customThis material was used directly in the next step without further purification
Sources & evidence
- ORD record
- ord-81c0f26e3e61450391cbf1f68bd039c7
- Source dataset
- uspto-grants-2013_03
- Patent number
- US08389549B2
Reaction notes
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