【摘要】 萘普生是一种非常重要而且有效的非甾体类消炎药,广泛应用于治疗疼痛、发热等症状.文章考察了新型手性N杂双膦配体(BIQAP)在不对称催化氢化制备萘普生中的应用研究,通过配体与金属钌形成手性催化剂,经过一系列条件的筛选,结果表明,在32℃、10 MPa H2、甲醇做溶剂、三乙胺做助剂的条件下,Ru(RBIQAP)(OAc)2能够有效地催化萘普生前体2-(6’-甲氧基-2’-萘基)丙烯酸,并取得了较高的收率(99%)和良好的对映选择性(81.7%ee).更多还原

【Abstract】 Naproxen is one of the important and effective nonsteroidal antiinflammatory drugs and widely used in pain and fever treatment. A novel chiral biphosphine ligands 6,6’-bis( diphenylphosphino)-5,5’-biquinoline( BIQAP) coordinate with Ru were successfully applied in asymmetric catalytic hydrogenation of 2-( 6’-methoxy-2’-naphthyl) propenoic Acid in this paper. After a series of experiments,the results show that in the condition of32 ℃,10 MPa H2,methanol as the solvent,the additive is Et3 N,Ru( R-BIQAP)( OAc)2as the catalyst. Optically pure naproxen with up to 81. 7% enantiomeric excess were obtained in high yield( 99%).更多还原