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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1773088Generated: November 3, 2026

Pyridine → (2S)-2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acid

https://huagongshe.com/reaction/1773088

Reaction equation

Participants

RoleNameHCIDCharge
ReactantPyridineHCID 1049—
Reactant3-Amino-5-chloro-2-hydroxybenzenesulfonic acidHCID 6927—
ReactantTriphosgeneHCID 94429—
Reactant(S)-tert-Butyl 3-amino-2-((tert-butoxycarbonyl)amino)propanoate hydrochlorideHCID 86679032—
SolventDichloromethaneHCID 6344—
Product(2S)-2-amino-3-{[(5-chloro-2-hydroxy-3-sulfophenyl)carbamoyl]amino}propanoic acidHCID 53377991—

Reaction Steps

297 mg (1 mmol) of 3-amino-N-(tert-butoxycarbonyl)-L-alanine tert-butylester hydrochloride, 223 mg (1 mmol) of 3-amino-5-chloro-2-hydroxybenzenesulfonic acid and 100 mg (0.33 mmol) of triphosgene were suspended in methylene chloride (3 ml), added with 0.8 ml of pyridine, and stirred at room temperature overnight. The solvent was distilled away, and the resultant residue was purified by employing purification step A to obtain the title compound in protected form. To the resulting protected form, 3 ml of trifluoroacetic acid was added, and the resultant was stirred for 5 hours. Subsequently, the solvent was distilled away and the obtained residue was purified using purification step A to obtain the title compound.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09253997B2
Source datasetuspto-grants-2016_02
ORD IDord-6da356e5e2dd435193d4a9503209f595
Source noteuspto-grants-2016_02