The Direct Synthesis of Unsymmetrical Vicinal Diamines from Terminal Alkynes: A Tandem Sequential Approach for the Synthesis of Imidazolidinones
作者:Laurel Schafer、Alison Lee、Melanie Sajitz
DOI:10.1055/s-0028-1083279
日期:2009.1
reaction is used in the synthesis of unsymmetrical vicinal diamines via the one-pot synthesis of α-cyanoamines. This methodology is further applied to the efficient synthesis of imidazolidinones. An easy-to-use bis(amidate)titanium precatalyst permits efficient approaches to heterocyclic chemistry from terminal alkynes. hydroamination - titanium - amines - heterocycles - tandem reactions
The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.
US7459479B2
申请人:——
公开号:US7459479B2
公开(公告)日:2008-12-02
N-Heterocyclic carbene–gold(I)-catalyzed carboheterofunctionalization of alkenes with arylboronic acids
作者:Shifa Zhu、Lijuan Ye、Wanqing Wu、Huanfeng Jiang
DOI:10.1016/j.tet.2013.09.097
日期:2013.12
A new approach to the synthesis of pyrrolidine, tetrahydrofuran, and imidazolidin-2-one via N-heterocyclic carbene–gold(I)-catalyzed intramolecular amino- or oxyarylation reactions from a wide variety of alkene substrates such as N-allyl amides, alcohols, carboxylic acids, and ureas in the presence of Selectfluor under mild conditions has been developed.