O-苄基-L-酪氨酸合成工艺改进

Improved Synthesis Process of O-Benzyl-L-Tyrosine

O -苄基 -L -酪氨酸是合成新型抗糖尿病药物PPARγ/α激动剂手性中间体S(- ) 3- (4-羟基苯基 ) - 2 -乙氧基丙酸乙酯的重要原料。本文在氢氧化钠作用下 ,L -酪氨酸、硫酸铜、溴化苄反应得到O -苄基酪氨酸铜配合物 ,然后采用EDTA— 2Na一锅法的后处理新工艺 ,得到O -苄基 -L -酪氨酸。该后处理方法 ,省去了用稀盐酸—氨水或稀盐酸—乙醇钠反复处理的麻烦 ,且产物无需重结晶 ,收率提高了 2 2 .6 %。

O-benzyl-L-tyrosine which was an important material for S(-)3-(4-hydrogen)phenyl-2-ethoxylpropionate,a chiral intermediate for new antidiabetic drug,was synthesized by L-tyrosine,copper sulfate and benzyl bromide.After the former troublesome method which required handling the copper chelate with dilute hydrochloride and ammonium or dilute hydrochloride and sodium ethylate again and again,O-Benzyl-L-Tyrosine was gotten with EDTA-2Na in one-pot method.The new method got high purification without recrystalization.The yield was increased by 22.6%.