反应详情

To a 2 dram vial equipped with a stir bar was added 2,4-dichloro-6-methylpyridine (29 mg, 0.18 mmol), 5-(tributylstannyl)thiazole (66 mg, 0.18 mmol), CuI (8 mg, 0.04 mmol), CsF (81 mg, 0.53 mmol), and Pd(PPh3)4 (10 mg, 8.9 μmol). The vial was capped with a septum screw-cap and then placed under N2 atmosphere. To the vial was added degassed DMF (1 mL). The vial was placed in a 80° C. heating block with stirring for 1 hour. The mixture was allowed to cool to room temperature and was then directly purified via C18 chromatography (water:MeOH w/0.1% TFA) to afford 5-(4-chloro-6-methylpyridin-2-yl)thiazole as a white solid. MS: MS m/z 211.1 (M++1). This material was directly carried forward into step 2.

1. customTo a 2 dram vial equipped with a stir bar
2. customThe vial was capped with a septum
3. customscrew-cap
4. additionTo the vial was added
5. customdegassed DMF (1 mL)
6. customwas placed in a 80° C.
7. temperatureheating block
8. customwas then directly purified via C18 chromatography (water:MeOH w/0.1% TFA)