ArticleChemical science2021
Rapid synthesis of pomalidomide-conjugates for the development of protein degrader libraries.
Article in Chemical science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 51 citations in OpenAlex.
- Alkyne Two-Phase Strategy: Rapid Generation of TK-285-Derived PROTACs as BRD4 Degraders.Journal of medicinal chemistry · 2026Article
- Accelerated synthesis of immunomodulatory imide drugs and their derivatives via continuous flow chemistry.Communications chemistry · 2026Article
- Lessons learned in linking PROTACs from discovery to the clinic.Nature reviews. Chemistry · 2026Review
- Synthesis, biological evaluation and clinical trials of Cereblon-based PROTACs.Communications chemistry · 2025Review
- Application of a bivalent "click" approach to target tyrosyl-DNA phosphodiesterase 1 (TDP1).RSC medicinal chemistry · 2025Article
- Property-based optimisation of PROTACs.RSC medicinal chemistry · 2025Article
- Harnessing Oxetane and Azetidine Sulfonyl Fluorides for Opportunities in Drug Discovery.Journal of the American Chemical Society · 2024Article
- Design, Synthesis, and Biological Evaluation of Selective TBL1X Degraders.ACS medicinal chemistry letters · 2024Article
- Preparation of von Hippel-Lindau (VHL) E3 ubiquitin ligase ligands exploiting constitutive hydroxyproline for benzylic amine protection.RSC advances · 2024Article
- Orthogonal IMiD-Degron Pairs Induce Selective Protein Degradation in Cells.bioRxiv : the preprint server for biology · 2024Article
- Article
- Rapid PROTAC Discovery Platform: Nanomole-Scale Array Synthesis and Direct Screening of Reaction Mixtures.ACS medicinal chemistry letters · 2023Article
- Leveraging Ligand Affinity and Properties: Discovery of Novel Benzamide-Type Cereblon Binders for the Design of PROTACs.Journal of medicinal chemistry · 2023Article
- A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs.Journal of medicinal chemistry · 2022Article
- Applications and Limitations of Oxime-Linked "Split PROTACs".Chembiochem : a European journal of chemical biology · 2022Article
- Development of Rapid and Facile Solid-Phase Synthesis of PROTACs via a Variety of Binding Styles.ChemistryOpen · 2022Article
- Identification of ligand linkage vectors for the development of p300/CBP degraders.RSC medicinal chemistry · 2022Article
- A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions.European journal of medicinal chemistry · 2022Article
- Construction of sulfur-containingRSC advances · 2022Article
- Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands.ACS medicinal chemistry letters · 2021Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Current methods for the preparation of heterobifunctional pomalidomide-conjugates rely on methods that are often low yielding and produce intractable byproducts. Herein we describe our strategy for the reliable and succinct preparation of pomalidomide-linkers which is essential to the formation of these conjugates. We present the preparation of 18 pomalidomide-linkers in high yield compared to current literature methods. Our findings show that secondary amines consistently afford greater yields than their primary counterparts, a trend that we were able to exploit in the synthesis of several new pomalidomide homo-dimers in enhanced yields compared to similar literature syntheses. This trend was further utilised to develop the first one-pot synthesis of JQ1-pomalidomide conjugates in yields up to 62%, providing a method that is suited to rapid preparation of conjugate libraries as is frequently required for the development of new protein degraders.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.