首次公开了通过非手性稳固的Pd 0配合物和简单的手性胺作为助催化剂的组合,线性醛类的第一个直接的分子间区域特异性和高对映选择性的α-烯丙基烷基化反应。将共催化的不对称化学选择性和区域特异性α-烯丙基烷基化反应与原位还原串联在一起,得到相应的2-烷基醇,其对映体比率很高(er高达98:2; er =对映体比率)。它也是有价值的2-烷基取代的半缩醛,2-烷基-丁烷-1,4-二醇和胺的快速入口。公开了具有生物活性的天然产物(例如,Arundic酸)的简明共催化不对称全合成。
Asymmetric Allylic Alkylation of Acyclic Allylic Ethers with Organolithium Reagents
作者:Manuel Pérez、Martín Fañanás-Mastral、Valentín Hornillos、Alena Rudolph、Pieter H. Bos、Syuzanna R. Harutyunyan、Ben L. Feringa
DOI:10.1002/chem.201202251
日期:2012.9.17
CuI/phosphoramidite‐catalyzed asymmetric allylic alkylation of allyl ethers with organolithiumreagents is reported (see scheme). The use of organolithiumreagents is essential for this catalytic CC bond formation due to their compatibility with different Lewis acids. The versatility of allylic ethers under the copper‐catalyzed reaction conditions with organolithiumreagents is demonstrated in the shortest
报道了用有机锂试剂对烯丙基醚进行的高效,区域和对映选择性的Cu I /亚磷酰胺催化的不对称烯丙基烷基化反应(参见方案)。由于与不同的路易斯酸具有相容性,因此使用有机锂试剂对于这种催化的CC键形成至关重要。(S)-戊二酸的最短合成证明了烯丙基醚在铜催化的条件下与有机锂试剂的多功能性。
[EN] PROCESSES FOR THE SYNTHESIS OF CHIRAL 1-ALKANOLS<br/>[FR] PROCÉDÉS DE SYNTHÈSE DE 1-ALCANOLS CHIRAUX
申请人:PURDUE RESEARCH FOUNDATION
公开号:WO2015106045A1
公开(公告)日:2015-07-16
The invention relates to highly enantioselective processes for the synthesis of chiral 1-alkanols via Zr-catalyzed asymmetric carboalumination of alkenes.
这项发明涉及通过锆催化的不对称烯烃碳铝化反应合成手性1-烷醇的高对映选择性过程。
PROCESSES FOR THE SYNTHESIS OF CHIRAL 1-ALKANOLS
申请人:PURDUE RESEARCH FOUNDATION
公开号:US20160332940A1
公开(公告)日:2016-11-17
The invention relates to highly enantioselective processes for the synthesis of chiral 1-alkanols via Zr-catalyzed asymmetric carboalumination of alkenes.
这项发明涉及通过Zr催化的不对称烯烃碳硼烷化反应合成手性1-烷醇的高对映选择性过程。
NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF
申请人:SU Zhengyu
公开号:US20160039879A1
公开(公告)日:2016-02-11
The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.
The invention relates to highly enantioselective processes for the synthesis of chiral 1-alkanols via Zr-catalyzed asymmetric carboalumination of alkenes.