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US 2025/0051287 A1Published application
Method for preparation of benzimidazole derivatives
AssigneeHk Inno.N Corporation
InventorsMin Kyoung LEE, Jae Hong KWEON, Jungeun LEE, Yeji PARK
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Abstract
The present invention relates to a method for preparing benzimidazole derivatives and a compound prepared thereby.
Claims28
A method for preparing benzimidazole derivatives, the method comprising:
- 1) preparing a compound represented by formula 2 below by reacting a compound represented by formula 3 below with a monovalent copper catalyst in a presence of a ligand represented by formula 4 below or a stereoisomer thereof;
- 2) preparing a compound represented by formula 5 below by reacting a compound represented by formula 2 below;
- and
- 3) preparing a compound represented by formula 1 below by reacting a compound represented by formula 5 below, acetyl chloride, and a compound represented by formula 6 below in a presence of a base,
- wherein,
- R1 is C1-4 alkyl or phenyl, wherein at least one H of the C1-4 alkyl and phenyl may be substituted with halogen or C1-4 alkyl,
- R2 is H, C1-4 alkyl or acetyl, wherein at least one H of the acetyl may be substituted with halogen,
- R3 and R4 are each independently selected from the group consisting of H, C1-4 alkyl and C3-7 cycloalkyl, or together form a 3- to 7-membered alicyclic ring, wherein at least one H of the C1-4 alkyl, C3-7 cycloalkyl and the formed 3- to 7-membered alicyclic ring may be substituted with halogen, and
- R5 is H, C1-4 alkyl or acetyl.
6 more elements
A compound represented by formula 1 below:
- wherein,
- R1 is C1-4 alkyl or phenyl, wherein at least one H of the C1-4 alkyl and phenyl may be substituted with halogen or C1-4 alkyl.
Dependencies are inferred from the claim text.