[EN] TRICYCLIC DEGRADERS OF IKAROS AND AIOLOS<br/>[FR] AGENTS DE DÉGRADATION TRICYCLIQUES D'IKAROS ET D'AIOLOS
申请人:C4 THERAPEUTICS INC
公开号:WO2020210630A1
公开(公告)日:2020-10-15
Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.
三环脑蛋白结合剂通过泛素蛋白酶体途径降解Ikaros或Aiolos以用于治疗应用的描述。
Direct Regioselective Synthesis of Tetrazolium Salts by Activation of Secondary Amides under Mild Conditions
作者:Veronica Tona、Boris Maryasin、Aurélien de la Torre、Josefine Sprachmann、Leticia González、Nuno Maulide
DOI:10.1021/acs.orglett.7b01004
日期:2017.5.19
Tetrazolium salts are biologically active molecules that have found broad applications in biochemical assays. A regioselective synthesis of tetrazolium salts is described through a formal (3 + 2) cycloaddition. The possibility of employing simple amides and azides as starting material and the mild conditions allow a broad functional group tolerance.
A 1,3-DIPOLE IN SULFILIMINE-PHOSPHINE SYSTEM (III) ACID ANHYDRIDE-, ESTER-, AND AMIDE-CONDENSATIONS BY SULFILIMINE-PHOSPHINE SYSTEM
作者:Tetsuo Aida、Naomichi Furukawa、Shigeru Oae
DOI:10.1246/cl.1975.29
日期:1975.1.5
Alkyl phenyl N-p-tosylsulfilimine and triphenylphosphine reacted with various carboxylic acids affording their anhydrides. The reaction was successfully extended to an ester- or amide-condensation reaction. These results can be interpreted by the initial formation of a 1,3-dipole between the sulfilimine and the phosphine.
been developed as chemoselective N-acylation reagents. Selective protection of primary amines in the presence of secondary amines, acylation of aliphatic amines in the presence of aryl amines, and monofunctionalization of primary-secondary diamines as well as selective N-acylation of amino alcohols using these reagents are described. All of the acylation reactions were carried out in water as a green
Some amide forming reactions involving boron reagents
作者:A. Pelter、T.E. Levitt、P. Nelsoni
DOI:10.1016/s0040-4020(01)92983-7
日期:1970.1
Attempts to evolve a new peptide synthesis using boron reagents have led to several new amide syntheses, involving either trialkylboranes. trialkoxyboranes, chlorodialkoxyboranes or dialkoxyboranes. The method using the readily available trimethoxyborane may be of general synthetic value. A new peptide synthesis was realized that gave a product of high optical purity but the low conversions achieved do not