IP Library Granted Patent US 12,202,800
Granted Patent B2
US 12,202,800 · App. 18/243,409 · Granted Jan 21, 2025

Method for producing amino acid derivatives

Inventors: Masato Murai (Tokyo, JP); Jun Takehara (Tokyo, JP); Daiki Okado (Tokyo, JP)
Assignee: API CORPORATION
C07D211/60
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Quick Facts
Patent No.
US 12,202,800
App. No.
18/243,409
Granted
Jan 21, 2025
Kind
B2
Abstract

A method for producing a compound represented by the formula (1): wherein LG is a leaving group, PG 1 is an amino-protecting group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s), comprising reacting a compound represented by the formula (6): with an amino group protecting agent to obtain a compound represented by the formula (7): or a salt thereof; reacting the aforementioned compound represented by the formula (7) with a lactonization agent to obtain a compound represented by the formula (8): reacting the aforementioned compound represented by the formula (8) with an esterification agent to obtain a compound represented by the formula (9): and reacting the aforementioned compound represented by the formula (9) with a leaving group introduction agent.

Claims (24)

1. A method for producing a compound represented by the formula (1):

wherein LG is a leaving group, PG 1 is an amino-protecting group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s),

comprising

reacting a compound represented by the formula (6):

with an amino group protecting agent to obtain a compound represented by the formula (7):

wherein each symbol is as defined above, or a salt thereof;

reacting the aforementioned compound represented by the formula (7) with a lactonization agent to obtain a compound represented by the formula (8):

wherein each symbol is as defined above;

reacting the aforementioned compound represented by the formula (8) with an esterification agent to obtain a compound represented by the formula (9):

wherein each symbol is as defined above; and

reacting the aforementioned compound represented by the formula (9) with a leaving group introduction agent.

2. A method for producing a compound represented by the formula (1):

wherein LG is a leaving group, PG 1 is an amino-protecting group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s),

comprising

reacting a compound represented by the formula (8):

wherein PG 1 is as defined above,

with an esterification agent to give a compound represented by the formula (9):

wherein each symbol is as defined above; and

reacting the aforementioned compound represented by the formula (9) with a leaving group introduction agent.

3. A compound represented by the following formula (1a) or (1b):

wherein

Boc is a tert-butoxycarbonyl group,

Ac is an acetyl group, and

Ns is a p-nitrobenzenesulfonyl group.

Assignments (2)
MERGER Recorded Jul 22, 2026
From: API CORPORATION
To: UBE CORPORATION
Reel/Frame 075349/0889 →
CHANGE OF ADDRESS FOR ASSIGNEE Recorded Sep 8, 2023
From: API CORPORATION
To: API CORPORATION
Reel/Frame 064845/0353 →
Priority Claims (1)
JP 2018-177774 · Sep 21, 2018 · national
Continuity (2)
Division 17277456
Related Publication 20240002340A1 · Jan 4, 2024
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