(R)-沙丁胺醇的化学不对称法合成

Synthesis of (R)-Albuterol with Chemical Asymmetric Method

采用化学不对称法合成(R)-沙丁胺醇.以1-(4-羟基-5-羟甲基苯基)-氨基乙酮为原料,通过CuI催化发生偶联反应,再通过以(-)-Ipc_2BCl作为还原剂对映选择还原羰基,最后生成(R)-沙丁胺醇,总产率93.1%.研究过程中考察了铜盐、配体、还原剂对各步合成的影响.

（R）-albuterol is synthetized with chemical asymmetric method.Taking 1-（4-hydroxy-5-hydroxymethyl phenyl）-amino acetophenone as raw material,coupling reaction reacts catalyzed by CuI;taking（-）-Ipc_2 BCl as reducing agent to make selective reduction in carbonyl group;（R）-albuterol is synthetized at last,and the overall yield of it is 93.1%.The effect of copper salts,ligands and reducing agents on each step of the synthesis is investigated.