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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1864618Generated: October 31, 2026

Triethylamine → (R)-2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-1-(4-methyl-2-oxo-2,3-dihydro-b enzoxazol-6-ylmethyl)-2-oxo-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate

https://huagongshe.com/reaction/1864618

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTriethylamineHCID 8471—
Reactant1-(4-Fluorophenyl)piperazineHCID 75260—
ReactantO-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborateHCID 2733207—
Reactant(R)-1-carboxy-2-(4-methyl-2-oxo-2,3-dihydrobenzoxazol-6-yl)-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylateHCID 68608307—
SolventDimethylformamideHCID 6228—
Product(R)-2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-1-(4-methyl-2-oxo-2,3-dihydro-b enzoxazol-6-ylmethyl)-2-oxo-ethyl 4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylateHCID 16734708—

Reaction Steps

234 mg (1.30 mmol) 1-(4-fluoro-phenyl)-piperazine were added to a solution of 600 mg (1.18 mmol) (R)-1-carboxy-2-(4-methyl-2-oxo-2,3-dihydrobenz-oxazol-6-yl)-ethyl 4-(2-oxo-1,2,4,5,-tetrahydro-1,3-benzodiazepin-3-yl)-piperidine-1-carboxylate, 417 mg (1.30 mmol) TBTU, 183 μL (1.30 mmol) triethylamine in 10 mL DMF and the reaction mixture was shaken at RT. The reaction solution was purified by HPLC without any further working up, the fractions containing the product were combined and lyophilised.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07625886B2
Source datasetuspto-grants-2009_12
ORD IDord-cee0bdd030a54af0aff2e3701691bcbc
Source noteuspto-grants-2009_12