Biarylphosphonite Gold(I) Complexes as Superior Catalysts for Oxidative Cyclization of Propynyl Arenes into Indan-2-ones
作者:Guilhem Henrion、Thomas E. J. Chavas、Xavier Le Goff、Fabien Gagosz
DOI:10.1002/anie.201301015
日期:2013.6.10
Striking gold: A series of variously functionalized propynyl arenes was smoothly converted into indan‐2‐ones by a new gold(I)‐catalyzed oxidative cyclization process. [LAu]NTf2 (Tf=trifluoromethanesulfonyl) is a superior catalyst both in terms of yield and kinetics for the present transformation.
打击金:通过新的金(I)催化的氧化环化工艺,一系列功能化的丙炔基芳烃被顺利转化为茚满-2-酮。就本转化而言,就收率和动力学而言,[ L Au] NTf 2(Tf =三氟甲磺酰基)是优良的催化剂。
METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG
申请人:Cayman Chemical Company, Incorporated
公开号:EP2928858A2
公开(公告)日:2015-10-14
[EN] METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG<br/>[FR] PROCÉDÉS DE SYNTHÈSE D'UN ANALOGUE DE PROSTACYCLINE
申请人:CAYMAN CHEMICAL CO INC
公开号:WO2014089385A2
公开(公告)日:2014-06-12
The present invention provides processes for preparing a prostacyclin analogue of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R10 is a linear or branched C1-6 alkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound.