萘普生是一种非常重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).
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 of 32 ℃,1 0 MPa H2 ,methanol as the solvent,the additive is Et3 N,Ru(R-BIQAP)(OAc)2 as the catalyst.Op-tically pure naproxen with up to 81 .7% enantiomeric excess were obtained in high yield (99%).