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Progress in Synthesis of Nebivolol

Tian Lei,Tao Jie,Li Jian(1.College of Material Science and Technology,Nanjing University of Aeronauticsand Astronautics,29 Yudao Street,Nanjing 210016;2.College of Bio&Chemical and Environmental Engineering,Nanjing Xiaozhuang University,Nanjing 211171)  
(S,R,R,R)-nebivolol is a novel and effective β1-adrenergic blocker with antihypertensive activity.The paper described five scheme to synthesize nebivolol,which was obtained with using p-fluoro-phenol or 6-fluro-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid or 6-fluro-3,4-dihydro-2H-1-benzopyran-2-carboxaldehyde as the starting material.While 6-fluro-3,4-dihydro-2H-1-benzopyran-2-carboxylic acid or 6-fluro-3,4-dihydro-2H-1-benzopyran-2-carboxaldehyde was obtained with using p-fluoro-phenol as the starting material.Different syntheses were compared in the paper.
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