반응 #2161592

반응 방정식

compound

1-{(S)-2-[(5-Bromo-pyrimidin-2-ylamino)-methyl]-pyrrolidin-1-yl}-1-[5-(4-fluoro-phenyl)-2-methyl-thiazol-4-yl]-methanone

lithium chloride

tetramethyl tin

→

title product

1-[5-(4-Fluoro-phenyl)-2-methyl-thiazol-4-yl]-1-{(S)-2-[(5-methyl-pyrimidin-2-ylamino)-methyl]-pyrrolidin-1-yl}-methanone

용매

dimethylformamide

반응 조건

후처리

1. 1
   기타The reaction was then evaporated
2. 2
   workup.ADDITIONdiluted with dichloromethane
3. 3
   여과filtered
4. 4
   세척the filtrate washed with water
5. 5
   기타dried
6. 6
   기타evaporated
7. 7
   세척Chromatography of the residue on silica gel, eluting with methanol-dichloromethane mixtures

실험 절차

To the compound of Example 194 (0.36 g) in dimethylformamide was added lithium chloride (0.096 g), tetramethyl tin (0.126 ml) and dichlorobis(triphenylphosphine) palladium (0) (0.035 g) and the resulting mixture heated at 100° C. under argon for 18 h. The reaction was then evaporated, diluted with dichloromethane, filtered and the filtrate washed with water, dried and evaporated. Chromatography of the residue on silica gel, eluting with methanol-dichloromethane mixtures, afforded the title product (0.2 g) as a yellow amorphous solid. Mass Spectrum (API+): Found 412 (MH+). C21H22FN5OS requires 411.

출처