O-对甲氧基苯基-N,N-二苄基酪氨酸乙酯的合成

Synthesis of Ethyl p-Methoxyphenyl-N,N-dibenzyl-tyrosine Ester

N,N-二苄基酪氨酸乙酯(2)与对溴苯甲醚(3)经偶联反应合成了O-对甲氧基苯基-N,N-二苄基酪氨酸乙酯,其结构经NMR,IR和MS表征。最佳反应条件为:210mmol,n(2)∶n(3)∶n(K3PO4)∶n(CuSO4.5H2O∶n(N,N-二甲基甘氨酸盐酸盐)=1.0∶1.3∶1.3∶0.2∶0.35,在DMF(50mL)中于100℃反应8h,产率54.7%,93.8%ee。

Ethyl p-methoxyphenyl-N,N-dibenzyl-tyrosine ester（1）was synthesized by the coupling reaction of ethyl N,N-dibenzyltyrosine ester（2）and p-bromophenyl methyl ether（3）.The structure was characterized by NMR,IR and MS.The optimal reaction conditions at 100 ℃ for 8 h in DMF（50 mL）were as follows：2 was 10 mmol,n（2）∶n（3）∶n（K3PO4）∶n（CuSO4·5H2O）∶n（Me2N CH2CO2H·HCl）was 1.0 ∶1.3 ∶1.3 ∶0.2 ∶0.35.The yield of 1 was 54.7% with 93.8%ee under the conditions.