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US 2026/0209169 A1Published application
New process for the manufacture of mdm2-p53 antagonists
AssigneeBoehringer Ingelheim International GmbH
InventorsJidong SHAO, Qing XIAO, Dihan ZHANG, Zhibin ZHU
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Abstract
This invention relates to a novel process for the synthesis of substituted aniline of formula (1) or salts thereof via hydroxy-indolinone of formula (13). The process of this invention is palladium free and uses oxygen as green and save oxidant for the copper promoted ring-opening of a hydroxy-indolinone bicycle to a tetra substituted aniline.
Claims14
A process for the manufacturing of a compound of formula (1)
- or a salt thereof,
- comprising the oxidative ring-opening of a compound of formula (13)
- wherein
- R* is a cleavable carboxyl protecting group, preferably an optionally substituted C1-6alkyl or an optionally substituted benzyl group, most preferably selected from the group consisting of methyl, ethyl, iso-propyl and benzyl, and
- PG is a suitable amino protective group, preferably a group —C(═O)—R, wherein R is R′ or —O—R′ and R′ is an optionally substituted linear, branched or cyclic aliphatic or aromatic group or combinations thereof, most preferably a protective group selected from the group consisting of acetyl (Ac) and tert-butyloxy carbonyl (Boc).
2 more elements
Dependencies are inferred from the claim text.