BARAN, PHIL,LI, CHAO,WANG, JIE,CHATTERJEE, ARNAB KUMAR,KUMAR, MANOJ,YU, SHAN,JOHNSON, KRISTEN ANN,QIN, TIAN,SHANG, MING
申请号：
CA3057443
公开号：
CA3057443A1
申请日:
2018.03.14
申请国别(地区):
CA
年份:
2018
代理人:
摘要：
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.
