2-(2-Iodo-3-methyl-benzoylamino)-indan-2-carboxylic acid ethyl ester → 2-[3-Methyl-2-(2-methyl-propenyl)-benzoylamino]-indan-2-carboxylic acid ethyl ester

Beteiligte Stoffe

Reaktionsschritte

To a solution of 2-(2-iodo-3-methyl-benzoylamino)-indan-2-carboxylic acid ethyl ester (400 mg, 0.89 mmol) and 2,2-dimethyethylenelboronic acid (133 mg, 1.34 mmol) in dioxane (15 mL) is added PdCl2(dppf) ([1,1′-bis(diphenylphosphine)ferrocene]-dichloropalladium(II), 73 mg, 8.9% mmol) and 2M aqueous solution of CsCO3 (1.34 mL, 2.67 mmol). The resulting reaction mixture is covered with argon and run in a microwave reaction: 110° C., 2 h. After concentration in vacuo, the residue is purified by flash column chromatography (120 g silica gel, gradient elution: 5-50% EtOAc in heptane) to give a pure product (134) as a pale yellow solid (523 mg, 78%).

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