通过衍生自芳基或烷基溴化物的格利雅试剂的反应,然后与芳族或脂族醛的反应以及随后用1,3-二碘的处理,可以有效地以高收率高效地制备各种二芳基酮,烷基芳基酮和二烷基酮。一锅法中的-5,5-二甲基乙内酰脲和K 2 CO 3。相同的处理的芳族溴化物轴承吸电子基团,如酯,腈,酮和硝基与我-PrMgCl·LiCl或PhMgCl代替Mg,也以良好的收率提供了相应的二芳基和烷基芳基酮。以上方法是用于制备各种带有富电子芳族基团和缺电子芳族基团的二芳基酮和烷基芳基酮以及二烷基酮的简单且实用的无过渡金属的方法。
[EN] BIFUNCTIONAL COMPOUNDS FOR THE TREATMENT OF CANCER<br/>[FR] COMPOSÉS BIFONCTIONNELS POUR LE TRAITEMENT DU CANCER
申请人:HOFFMANN LA ROCHE
公开号:WO2021083949A1
公开(公告)日:2021-05-06
The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).
Pharmaceutical use of [[[(3-pyridinyl)methylen]amino]oxy]alkanoic acids
申请人:Janssen Pharmaceutica N.V.
公开号:US04746671A1
公开(公告)日:1988-05-24
Novel [[[(3-pyridinyl)methylen]amino]oxy]alkanoic acids and esters, compositions containing the same, and methods of treating clinical conditions related with the production of thromboxane A.sub.2, prostacyclin and/or prostaglandins D.sub.2, E.sub.2 and F.sub.2.alpha..