1360616-36-9

Basic information

• Product Name: tert-butyl 4-(oxazol-5-yl)benzylcarbamate
• Synonyms: tert-butyl 4-(oxazol-5-yl)benzylcarbamate
• CAS NO: 1360616-36-9
• Molecular Weight: 274.32
• Mol File: 1360616-36-9.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: tert-butyl 4-(oxazol-5-yl)benzylcarbamate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl 4-(oxazol-5-yl)benzylcarbamate(1360616-36-9)
• EPA Substance Registry System: tert-butyl 4-(oxazol-5-yl)benzylcarbamate(1360616-36-9)

Safety Data

• Hazardous Substances Data: 1360616-36-9(Hazardous Substances Data)

Upstream product

• 156866-52-3 tert-butyl N-(4-formylbenzyl)carbamate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 87150-13-8 4-(oxazol-5-yl)benzonitrile 
• 105-07-7 4-cyanobenzaldehyde 
• 33233-67-9 4-(tert-Butoxycarbonylaminomethyl)benzoic acid 
• 38622-91-2 [(p-methylphenyl)sulfonylmethyl]isonitrile 
• 314732-37-1 tert-butyl 4-(methoxy(methyl)carbamoyl)benzylcarbamate 
• 56-91-7 p-aminomethylbenzoic acid 

Downstream Products

• 1360616-38-1 (4-(oxazol-5-yl)phenyl)methanamine trifluoroacetate salt 
• 1422984-95-9 N-(4-(oxazol-5-yl)benzyl)acetamide 
• 672324-91-3 [4-(1,3-oxazol-5-yl)phenyl]methanamine 

Relevant articles and documents

Compounds & Methods for the Enhanced Degradation of Targeted Proteins & Other Polypeptides by an E3 Ubiquitin Ligase

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.

Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities

E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-molecule ligands has been rewarded with limited success. The von Hippel-Lindau protein (pVHL) is the substrate recognition subunit of the VHL E3 ligase that targets HIF-1α for degradation. We recently reported inhibitors of the pVHL:HIF-1α interaction, however they exhibited moderate potency. Herein, we report the design and optimization, guided by X-ray crystal structures, of a ligand series with nanomolar binding affinities.

Targeting the von Hippel-Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction

E3 ubiquitin ligases, which bind protein targets, leading to their ubiquitination and subsequent degradation, are attractive drug targets due to their exquisite substrate specificity. However, the development of small-molecule inhibitors has proven extrao