反应详情

0.39 ml of n-butyllithium solution (1.6M in hexane) is added at −75° C. to a 0.5 M solution of zinc chloride in THF and the resulting mixture stirred for 30 min at room temperature. This solution is added via a syringe to a solution of 107 mg 3-iodo-2-(3-methoxy-6-pyridin-4-yl-pyridazin-4-yl)-1H-indole (9b) and 10 mg 1,1′-bis(diphenylphosphino)ferrocene-palladium(II)dichloride (1:1 complex with CH2Cl2) in THF and stirred for 4 h at 70° C. The reaction mixture is quenched by adding saturated NH4Cl-solution and extracted with ethylacete. The combined organic layers are dried over MgSO4, the solvens removed in vacuo. Reversed phase chromatography (RP18, water (0.05% HCOOH)/acetonitrile (0.05% HCOOH)) 30 mg product.

1. stirringstirred for 4 h at 70° C
2. customThe reaction mixture is quenched
3. additionby adding saturated NH4Cl-solution
4. extractionextracted with ethylacete
5. dry with materialThe combined organic layers are dried over MgSO4
6. customthe solvens removed in vacuo