The invention relates to an asymmetric
hydrogen transfer synthesis method for (R,R)-
formoterol, and relates to a novel method for synthesizing an optical pure beta 2-adrenoreceptor excitant, namely
formoterol. The method comprises: firstly, taking 4-hydroxyl-3 nitroacetophenone as a
raw material, using benzyl groups to protect phenolic hydroxyl groups, and obtaining alpha-bromo keto after bromination; secondly, taking (S,S)-Rh-PEG-BsDPEN as a catalyst and
formic acid and derivatives of the
formic acid as
hydrogen sources, and synthesizing chiral
alcohol intermediate by an asymmetric
hydrogen transfer method; thirdly, using (R)-alpha-methyl phenylethylamine and methoxyl
phenylacetone to generate
imine compounds, and obtaining
chiral amine intermediate through hydrogenation reduction under the
catalysis of Pt / C; and fourthly, reacting and
coupling the chiral
alcohol intermediate and the
chiral amine intermediate, removing protective groups, and obtaining the (R,R)-
formoterol. The invention uses the asymmetric
hydrogen transfer method and a
chiral auxiliary reagent to synthesize the (R,R)-formoterol, and has high yield and good ee value. Compared with a method for synthesizing chiral formoterol through chemical splitting, the method has the advantages of high total yield, mild
reaction conditions, low cost and so on, and is favorable for industrial production.