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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 494750Generated: October 30, 2026

Sodium Hydroxide → 3-(4-Amino-3-chloro-5-trifluoromethyl-phenyl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionic Acid

https://huagongshe.com/reaction/494750

Reaction equation

Participants

RoleNameHCIDCharge
ReactantSodium HydroxideHCID 14798—
ReactantEthyl 3-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionateHCID 22184546—
SolventEthanolHCID 702—
Product3-(4-Amino-3-chloro-5-trifluoromethyl-phenyl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionic AcidHCID 22184605—

Reaction Steps

To a solution of 13.00 g (22.34 mmol) ethyl 3-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-{[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-carbonyl]-amino}-propionate (Intermediate product 59) in 100 mL EtOH was added 45 mL aqueous NaOH (1 M) and the mixture was stirred for 16 hours at RT. EtOH was evaporated i. vac., 45 mL aqueous HCl (1M) was added and 15 minutes stirred. The precipitate formed was filtered off, washed with water and dried i. vac. at 75° C.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07538115B2
Source datasetuspto-grants-2009_05
ORD IDord-3c3f85dfbd5f4e409d5fca31e39f17ba
Source noteuspto-grants-2009_05