Selective desilylation of -butyldimethylsilyl ethers of phenols using potassium fluoride-alumina and ultrasound
摘要:
The use of potassium fluoride on basic alumina in acetonitrile with ultrasound for the selective deprotection of tert-butyldimethysilyl ethers of phenols is described. The method, which features a non-aqueous work-up, readily cleaves tert-butyldimethylsilyl ethers of phenols at room temperature, whereas tert-butyldimethylsilyl ethers of benzyl alcohols or 2-(trimethylsilyl)ethoxymethyl ethers of phenols are stable.
The present invention provides compounds, compositions thereof, and methods of using the same.
本发明提供了化合物、其组合物以及使用这些化合物的方法。
[EN] IRAK DEGRADERS AND USES THEREOF<br/>[FR] AGENTS DE DÉGRADATION D'IRAK ET LEURS UTILISATIONS
申请人:KYMERA THERAPEUTICS INC
公开号:WO2020264499A1
公开(公告)日:2020-12-30
The present invention provides compounds, compositions thereof, and methods of using the same. The compounds include an IRAK binding moiety capable of binding to IRAK4 and a degradation inducing moiety (DIM). The DIM could be DTM a ligase binding moiety (LBM) or lysine mimetic. The compounds could be useful as IRAK protein kinase inhibitors and applied to IRAK mediated disorders.
[EN] MITOTIC KINESIN INHIBITORS<br/>[FR] INHIBITEUR DE KINESINES MITOTIQUES
申请人:MERCK & CO INC
公开号:WO2003105855A1
公开(公告)日:2003-12-24
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Imidazole compounds having adenosine deaminase inhibitory activity represented by formula (I) wherein R1 is hydrogen, hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s); R2 is hydrogen or lower alkyl; R3 is hydroxy or protected hydroxy; R4 is cyano, (hydroxy)iminoamino(lower)alkyl, carboxy, protected carboxy, heterocyclic group optionally substituted with amino, or carbamoyl optionally substituted with suitable substituent(s); and —A— is —Q— or —O—Q—, wherein Q is single bond or lower alkylene, provided that when R2 is lower alkyl, then R1 is hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s), its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.
A direct and catalytic method is reported here for β‐arylation of N‐protected lactams with simple aryl iodides. The transformation is enabled by merging soft enolization of lactams, palladium‐catalyzed desaturation, Ar−X bond activation, and aryl conjugate addition. The reaction is operated under mild reaction conditions, is scalable, and is chemoselective. Application of this method to concise syntheses