On June 28, 2018, Grew, Andrew P.; Zimmermann, Kurt; Wang, Jing; Berlin, Michael; Dong, Hanqing; Ishchenko, Alexey; Qian, Yimin; Crews, Craig M.; Jaime-Figueroa, Saul; Burslem, George published a patent.Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate The title of the patent was Preparation of heterocyclic compounds as EGFR proteolysis targeting chimeric molecules and associated methods of use. And the patent contained the following:
The disclosure relates to bifunctional compounds of formula I, which find utility as modulators of receptor tyrosine kinase (RTK) proteins. The disclosure is directed to bifunctional compounds of formula I, which contain on one end a ligand which binds to an E3 ubiquitin ligase and on the other end a moiety which binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effectuate ubiquitination, and therefore, degradation (and inhibition) of the target protein. The disclosure exhibits a broad range of pharmacol. activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the disclosure. Compounds of formula I wherein ULM is a small mol. E3 ubiquitin ligase binding moiety; PTM is a small mol. receptor tyrosine kinase protein targeting moiety; L is a bond and a chem. linking moiety; and pharmaceutically acceptable salts, enantiomers, stereoisomers, solvates, polymorphs and prodrugs thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluate for their EGFR inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of in the range of 0.0021 μM to 12 μM. The experimental process involved the reaction of tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate(cas: 882518-89-0).Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate
The Article related to heterocycle preparation egfr proteolysis targeting chimeric mol, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Name: tert-Butyl 2-(2-(2-(tosyloxy)ethoxy)ethoxy)acetate
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