3-(4-Methoxybenzoyl)-4,5,6,7-tetrahydro-1-benzothiophen-2-amine → Cyclopropyl-[4-(4-methoxy-phenyl)-2-methyl-5,6,7,8-tetrahydro-benzo[4,5]thieno[2,3-b]pyridin-3-yl)-methanone

참여 물질

반응 조건

반응 단계

To a stirred solution of 60 mg (0.21 mmol) (2-amino-4,5,6,7-tetrahydro-benzo[b]thiophen-3-yl)-(4-methoxy-phenyl)-methanone (the preparation of which is described in example 8) in 2 ml acetic acid was added 35 mg (0.28 mmol) of 1-cyclopropyl-butane-1,3-dione and one drop of sulfuric acid. The mixture was then stirred at 100° C. for 10 minutes in a microwave and then concentrated in vacuo. Preparative HPLC (30% CH3CN/H20) afforded 25 mg (32%) cyclopropyl-[4-(4-methoxy-phenyl)-2-methyl-5,6,7,8-tetrahydro-benzo[4,5]thieno[2,3-b]pyridin-3-yl)-methanone as a light brown oil. ES-MS m/e (%): 378 (M+H+, 100).

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