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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 57064Generated: October 30, 2026

5-amino-2H-1,3-benzodiazol-2-one → 2-{4-[5-Chloro-2-(difluoromethoxy)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}-4-methoxy-N-(2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)butanamide

https://huagongshe.com/reaction/57064

Reaction equation

Participants

RoleNameHCIDCharge
Reactant5-amino-2H-1,3-benzodiazol-2-oneHCID 15250547—
Reactant2-{4-[5-Chloro-2-(difluoromethoxy)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}-4-methoxybutanoic acidHCID 117622801—
Product2-{4-[5-Chloro-2-(difluoromethoxy)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}-4-methoxy-N-(2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)butanamideHCID 117623002—

Reaction Steps

76 mg (purity 82%, 0.15 mmol) of 2-{4-[5-chloro-2-(difluoromethoxy)phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl}-4-methoxybutanoic acid (racemate) and 25 mg (0.17 μmol, 1.1 eq.) of 5-aminobenzimidazolone were reacted according to General Method 1. The crude product was purified by preparative HPLC (Reprosil C18, water/acetonitrile gradient). Yield: 37 mg (45% of theory)

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09434690B2
Source datasetuspto-grants-2016_09
ORD IDord-cf8dd5a071824f4b840d2b434023361e
Source noteuspto-grants-2016_09