巴格列酮的合成

Synthesis of Balaglitazone

以1H-苯并[d][1,3]噁嗪-2,4-二酮与甲胺反应得到2-氨基-N-甲基苯甲酰胺,与氯乙酰氯环合后经醚化反应、Knoevenagel反应及催化氢化得到糖尿病治疗药巴格列酮,总收率约48%。

Balaglitazone, an antihyperglycemic agent, was synthesized from 1H-benzoEd] [1,3] oxazine-2,4- dione with methylamine to give 2-amino-N-methylbenzamide, which underwent cyclization with 2-chloroacetyl chloride, followed by etherification, Knoevenagel reaction and catalytic hydrogenation with an overall yield of about 48 %.