The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Nov. 02, 2021
Filed:
Mar. 14, 2018
The Scripps Research Institute, La Jolla, CA (US);
Phil Baran, San Diego, CA (US);
Chao Li, San Diego, CA (US);
Jie Wang, San Diego, CA (US);
Arnab Kumar Chatterjee, San Diego, CA (US);
Manoj Kumar, San Diego, CA (US);
Shan Yu, San Diego, CA (US);
Kristen Ann Johnson, Santee, CA (US);
Tian Qin, Dallas, TX (US);
Ming Shang, San Diego, CA (US);
THE SCRIPPS RESEARCH INSTITUTE, La Jolla, CA (US);
Abstract
The invention is directed to methods of converting a carboxylic acid group in a compound, via a redox active ester, to a corresponding boronic ester by treatment with bis(pinacolato)diboron-alkyllithium complex in the presence of a ligand, a Ni(ll) salt or a copper salt, and an Mg(ll) salt, in the presence of an alkyllithium or a lithium hydroxide or alkoxide salt. The product pinacolato boronate ester can be cleaved to provide a boronic acid. The invention is also directed to methods of preparing various compounds of medical value comprising boronic acid groups, and to novel boronic-acid containing compounds of medicinal value, including an atorvastatin boronic acid analog, a vancomycin aglycone boronic acid analog, and boronic acid containing elastase inhibitors mCBK319, mCBK320, mCBK323, and RPX-7009.