摘要
7-氨基-3(-1-吡啶甲基)头孢烯酸(7-APCA)氯化物是合成头孢他啶的重要中间体。以GCLE为原料经过3步反应,首先GCLE和NaI反应制备碘化物,进一步和吡啶反应得到3位取代产物,然后经过脱除7位和4位的保护基得到7-APCA的卤化物,总收率为77%,各化合物均通过1H-NMR确证结构。
7-amino-3(1-pyridiniumaethyl)-3-cephem-4-carboxylic acid halide was an important intermediate of ceftazidime, The 7-APCA was obtained from GCLE in 3 steps. Firstly reaction of GCLE with NaI gave the corresponding iodide intermediate , which reacted with pyridine to afford the substitution compound at 3-position. Then the protecting groups at 7-position and 4-position were removed to give 7-a mino-3- (1-pyridiniumaethyl)-3-cephem-4-carboxylic acid halide . The total yield is 77% and the products Were confirmed by ^1H-NMR.
出处
《河北化工》
2007年第1期18-19,共2页
Hebei Chemical Industry