Methylamine → 6-Bromo-8-isopropyl-4-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one
Reaction equation
[Br:1][C:2]1[C:15](=[O:16])[N:14]([CH:17]([CH3:19])[CH3:18])[C:5]2[N:6]=[C:7](S(C)=O)[N:8]=[C:9]([CH3:10])[C:4]=2[CH:3]=1.[CH3:20][NH2:21]>O1CCOCC1>[Br:1][C:2]1[C:15](=[O:16])[N:14]([CH:17]([CH3:19])[CH3:18])[C:5]2[N:6]=[C:7]([NH:21][CH3:20])[N:8]=[C:9]([CH3:10])[C:4]=2[CH:3]=1Participants
4
Conditions
- Temperature
- 110 °C
Procedure
To a stirred solution of 6-bromo-8-isopropyl-4-methyl-2-(methylsulfinyl)pyrido[2,3-d]pyrimidin-7(8H)-one (175 mg, 0.508 mmol) in 1,4-dioxane (2.5 mL) was added methyl amine (0.80 mL, 2.0 M in THF, 1.6 mmol). The mixture was sealed and heated at 110° C. microwave for 15 min. The solvent was evaporated and the crude product was washed with EtOAc/Hexane to give the title compound (158 mg, 76%).
Workup
- customThe mixture was sealed
- customThe solvent was evaporated
- washthe crude product was washed with EtOAc/Hexane
Sources & evidence
- ORD record
- ord-3038bd47164441d1b74eb75169c64dd3
- Source dataset
- uspto-grants-2010_04
- Patent number
- US07696213B2
Reaction notes
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