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Green Synthesis of (R)-Terbutaline for Recyclable Catalytic Asymmetric Transfer Hydrogenation in Ionic Liquids

机译:(R)-特布他林的绿色合成,用于离子液体中的可循环催化不对称转移加氢

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We synthesize optically active ( R )-terbutaline 2 , which is an anti-asthmatic drug, through recyclable catalytic asymmetric transfer hydrogenation (RCATH). Various chloroketones 4 were prepared and RCATH was performed on them. The products exhibit moderate to high enantioselectivity. In particular, the hydrogenation of acyl substituted substrates 4c yields chiral secondary alcohols 5c in good yield and enantioselectivity. Furthermore, ( R )-terbutaline 2 can be synthesized in one step from the resulting secondary alcohol 5 without racemization.
机译:我们通过可循环的催化不对称转移氢化(RCATH)合成了光学活性(R)-叔丁胺2,这是一种抗哮喘药。制备了各种氯酮4并对其进行了RCATH。产物表现出中等至高对映选择性。特别地,酰基取代的底物4c的氢化以良好的产率和对映选择性产生手性仲醇5c。此外,(R)-叔丁胺2可以在不消旋的情况下由所得仲醇5一步合成。

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