反应详情

To a solution of 0.25 g (0.69 mMol) 4-(2-amino-4-methoxy-benzothiazol-7-yl)-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester in 10 ml THF were added 0.26 ml ethyl diisopropyl amine and 0.16 g (0.76 mMol) 2-chloro-isonicotinoyl chloride, dissolved in 5 ml of dichloro methane. The reaction mixture was stirred at room temperature for 16 h. Then 5 ml methanol were added. The solvent was evaporated to dryness, the residue taken up in ethyl acetate and washed with water and brine. The organic phase was dried over sodium sulfate and evaporated to dryness in vacuo. The residue was subjected to column chromatography (ethyl acetate/hexane 1:1) to yield 0.308 g (89%) of 4-{2-[(2-chloro-pyridine-4-carbonyl)-amino]-4-methoxy-benzothiazol-7-yl}-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester as a yellow foam. ES-MS m/e (%): 501 ([M+H]+, 100).

1. customThe solvent was evaporated to dryness
2. washwashed with water and brine
3. dry with materialThe organic phase was dried over sodium sulfate
4. customevaporated to dryness in vacuo