(R)-1-(4-苄氧基-3-硝基苯基)-2-溴乙醇的合成

Synthesis of (R)-1-(4-Benzyloxy-3-nitrophenyl)-2-bromoethanol

4-羟基-3-硝基苯乙酮经O-苄基化、溴化、还原制得1-(4-苄氧基-3-硝基苯基)-2-溴乙醇,然后酶促拆分得(R,R)-型福莫特罗的关键中间体(R)-1-(4-苄氧基-3-硝基苯基)-2-溴乙醇,总收率约25%。

4-Hydroxy-3-nitroacetophenone was performed to undergo O-benzytation, bromination and reduction to give 1-（4-benzyloxy-3-nitrophenyl）-2-bromoethanol, from which （R）-1-（4-benzyloxy-3-nitrophenyl）-2- bromoethanol, the key intermediate of （R,R）-formoterol, was obtained via enzymatic resolution with an overall yield of about 25 %.