highly effective C−O coupling reaction of (hetero)aryl electrophiles with primary and secondary alcohols is reported. Catalyzed by a NiII‐arylcomplex under long‐wave UV (390–395 nm) irradiation in the presence of a soluble amine base without any additional photosensitizer, the reaction enables the etherification of aryl bromides and arylchlorides as well as sulfonates with a wide range of primary
据报道,(杂)芳基亲电试剂与伯醇和仲醇的高效C-O偶联反应。在可溶性胺碱的存在下,在没有任何其他光敏剂的情况下,在长波紫外线(390–395 nm)辐射下,由Ni II-芳基络合物催化,该反应可以使芳基溴化物和芳基氯化物以及磺酸盐与多种伯和仲脂族醇,可提供合成上重要的醚。分子内CO偶联也是可能的。该反应似乎通过Ni I -Ni III催化循环进行。
In the first communication the synthetic methods are described for preparing aromatic analogues of juvenile hormone like activity. The para-substituted 2-methyl-cinnamic acid derivatives are formed by a Friedel-Crafts acylation of a phenol, followed by the Wadsworth-Emmons (Wittig-Horner)-Reaction with the corresponding phosphonates. More than 120 compounds are listed.
Pyrone derivatives as protease inhibitors and antiviral agents
申请人:Warner-Lambert Company
公开号:US05808062A1
公开(公告)日:1998-09-15
The present invention relates to novel tri- and tetrasubstituted pyrones and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The pyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized pyrones and of related structures.
Reported herein is a ligand-enabled gold-catalyzed C(sp2)–O cross-coupling reaction of aryl iodides and aliphaticalcohols. The synthesis of a variety of aryl alkyl ethers including complex biomolecules and various medicinally relevant motifs has been achieved to demonstrate the usefulness of the method. The importance of gold catalysis has been highlighted by overcoming the selectivity issues that