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Solid‐Phase Synthesis of PROTACs and SNIPERs on Backbone Amide Linked (BAL) Resin.

Authors :
Hales, Liam Thomas
Thompson, Philip Evan
Source :
Chemistry - A European Journal; 10/9/2023, Vol. 29 Issue 56, p1-10, 10p
Publication Year :
2023

Abstract

Developing straightforward but flexible approaches to PROTAC synthesis that can incorporate the structural elements of emerging designs can improve the quality and efficiency of PROTAC development. Solid‐phase approaches could offer many advantages over conventional PROTAC synthesis if diverse chemistries and topographies can be incorporated. We have exploited the backbone‐amide‐linked (BAL) resin to employ an array of solid‐phase organic reactions, providing access to VHL‐ and IAP‐targeting degraders using the BRD4‐targeting JQ1 conjugates as examples. [ABSTRACT FROM AUTHOR]

Subjects

Subjects :
SOLID-phase synthesis
SNIPERS
SPINE

Details

Language :
English
ISSN :
09476539
Volume :
29
Issue :
56
Database :
Complementary Index
Journal :
Chemistry - A European Journal
Publication Type :
Academic Journal
Accession number :
172895121
Full Text :
https://doi.org/10.1002/chem.202301975