反应详情

0.30 g (0.60 mMol) 4-{2-[(2-chloro-pyridine-4-carbonyl)-amino]-4-methoxy-benzothiazol-7-yl}-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester were heated to 130° C. for 24 h in 1 ml morpholine and 0.39 g (1.2 mMol) cesium carbonate. The morpholin has been removed in vacuo. The residue has been triturated in ethyl acetate and subsequently subjected to column chromatography (ethyl acetate) to yield 0.15 g (45%) 4-{4-methoxy-2-[(2-morpholin-4-yl-pyridine-4-carbonyl)-amino]-benzothiazol-7-yl}-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester as a yellow foam. ES-MS m/e (%): 552 ([M+H]−, 100).

1. customThe morpholin has been removed in vacuo
2. customThe residue has been triturated in ethyl acetate