反应详情

3-pyridylboronic acid (127.3 mg, 1.036 mmol), 4-bromo-3-methyl-isothiazol-5-amine (100 mg, 0.518 mmol), Na2CO3 (777 μL of 2 M, 1.554 mmol), palladium triphenylphosphane (29.93 mg, 0.0259 mmol) in dioxane (6 mL) was heated at 110° C. in a microwave for 30 min. The mixture was concentrated in vacuo and the residue was loaded on a SCX column, washed with DCM/MeOH mixtures before the product was eluted with a 2M solution of ammonia in MeOH. The eluent was concentrated in vacuo to yield 3-methyl-4-(pyridin-3-yl)isothiazol-5-amine as a pale yellow oil that was used in next step without further purification. MS (ES+) 192.0.

1. concentrationThe mixture was concentrated in vacuo
2. washwashed with DCM/MeOH mixtures before the product
3. washwas eluted with a 2M solution of ammonia in MeOH
4. concentrationThe eluent was concentrated in vacuo