2-{4-[2-(吩噁嗪-10-基)乙氧基]苄基}-丙二酸二甲酯的合成

Synthesis of 2-{4-[2-(phenoxazin-10-yl)ethoxyl]-benzyl}-malonic acid Dimethyl Ester

2-{4-[2-(吩噁嗪-10-基)乙氧基]苄基}-丙二酸二甲酯是一种对Ⅱ型糖尿病有较高活性的化合物,活性较市场上药效最好的罗格列酮高,且具有PPARα、PPARγ双活性。文献报道的合成方法,使用了2溴乙醇、对卞氧基苯甲醛等价格昂贵,不易获得的原料,且反应过程需要高压条件。作者引入了相转移催化方法,所用原料为1,2二溴乙烷等,价格便宜,且易于获得,反应条件为常温常压,降低了生产成本。

2-{4-[2-(Phenoxazin-10-yl)ethoxyl]-benzyl}-malonic acid dimethyl ester,an active compound against typeⅡdiabetes,is more potent than rosiglitazone,the most potent drug in the market.This compound has dual activities of PPAR-αand PPAR-γ.The reported synthetic method is laborious and the reagents,such as 2-bromoethanol and 4-benzyloxybenzaldehyde,are not easily available and too expensive.Phase trsnsfer catalysis is introduced to our method.Compared with the reported method,our method has the advantages of mild reaction conditions of room temperature and normal pressure and the reagents,such as 1,2-dibromoethane,are easily available and cheap,thus the cost of production is reduced.