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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1629753Generated: November 1, 2026

Lithium Hydroxide → 1-{2-Chloro-5-[(S)-1-(4-chloro-3-methyl-phenyl)-2,2,2-trifluoro-ethylamino]-benzyl}-3-methyl-azetidine-3-carboxylic acid

https://huagongshe.com/reaction/1629753

Reaction equation

Participants

RoleNameHCIDCharge
ReactantLithium HydroxideHCID 3939—
Reactant(S)-1-(4-chloro-3-methyl-phenyl)-2,2,2-trifluoro-ethylamine hydrochlorideHCID 57517340—
ReactantMethyl 3-methylazetidine-3-carboxylate hydrochlorideHCID 67329141—
Product1-{2-Chloro-5-[(S)-1-(4-chloro-3-methyl-phenyl)-2,2,2-trifluoro-ethylamino]-benzyl}-3-methyl-azetidine-3-carboxylic acidHCID 53339656—

Reaction Steps

The title compound was prepared according to Scheme 4 following a procedure analogous to Example 61 using 3-methyl-azetidine-3-carboxylic acid methyl ester hydrochloride (INT 14) in step 1 and (S)-1-(4-chloro-3-methyl-phenyl)-2,2,2-trifluoro-ethylamine hydrochloride in step 2, followed by a LiOH-mediated ester cleavage.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08791100B2
Source datasetuspto-grants-2014_07
ORD IDord-8c83f63bb9b54a9f8fa05ac593c23d00
Source noteuspto-grants-2014_07