Deconstructive Diversification Of Cyclic Amines Useful For Proline Tagging

Tech ID: 31707 / UC Case 2018-187-0

Patent Status

Patent Pending

Brief Description

A deconstructive strategy to transform saturated nitrogen heterocycles such as piperidines and pyrrolidines into halogen-containing acyclic amine derivatives through sequential Csp3–N/Csp3–Csp3 single bond cleavage followed by Csp3–halogen bond formation. The resulting acyclic haloamines serve as versatile intermediates that are expediently transformed into a variety of structural motifs through substitution reactions. In this way, skeletal remodeling, which constitutes a scaffold hop, can be achieved. The value of this deconstructive strategy has been demonstrated through the late-stage diversification of proline-containing peptides, thus achieving late-stage proline tagging.

Suggested uses

Tagging of prolines on proteins and peptides to allow the addition of payloads and diversification of peptides in DNA encoded libraries. This is an area of interest to pharmaceutical companies.

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Inventors

  • Sarpong, Richmond

Other Information

Keywords

DNA encoded libraries, protein tagging, peptide modification

Categorized As

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