有机催化的苄醇与吡唑啉酮亚胺的不对称加成反应  

Organocatalytic Asymmetric Addition of Phenylmethanol to Pyrazolinone Ketimines

作　　者：周扬 周鸣强[1] 袁伟成[1] ZHOU Yang;ZHOU Ming-qiang;YUAN Wei-cheng(National Engineering Research Center of Chiral Drugs,Chengdu Institute of Organic Chemistry,Chinese Academy of Sciences,Chengdu 610041,China)

机构地区：[1]中国科学院成都有机化学研究所手性药物国家工程研究中心

出　　处：《合成化学》2019年第11期873-877,共5页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(21602217);中国科学院西部之光青年学者项目

摘　　要：以金鸡纳碱衍生的双功能方酰胺为催化剂,催化苄醇与吡唑啉酮亚胺的不对称加成反应,以高达85%的收率和92%ee合成了12个结构新颖的含有吡唑啉酮骨架的N,O-缩醛类手性化合物,其结构经1H NMR,13C NMR,HR-MS(ESI-TOF)及X-ray表征。An organocatalytic asymmetric addition of phenylmethanol with pyrazolone derived N-Boc ketimines catalyzed by cinchona-derived bifunctional squaramid has been developed.With this protocol,a series of chiral compounds bearing pyrazolone and N,O-acetal skeletons were obtained in good yields(up to 85%)and high enantioselectivities(up to 92%ee).The structures were characterized by 1 H NMR,13 C NMR,HR-MS(ESI-TOF)and X-ray.

关 键 词：N O-缩醛 有机催化 苄醇 吡唑啉酮亚胺 合成 

分 类 号：O621.3[理学—有机化学] O626[理学—化学]