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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1266867Generated: November 4, 2026

Trifluoroacetic acid → 4-[3-(5-Hydroxymethyl-isoxazol-3-yl)-phenyl]-7-morpholin-4-yl-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

https://huagongshe.com/reaction/1266867

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant(RS)-[5-Morpholin-4-yl-2-(3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-isoxazol-3-yl]-phenyl}-propionylamino)-4-trifluoromethyl-phenyl]-carbamic acid tert.-butyl esterHCID 86586983—
SolventDichloromethaneHCID 6344—
Product4-[3-(5-Hydroxymethyl-isoxazol-3-yl)-phenyl]-7-morpholin-4-yl-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 18548872—

Reaction Steps

The title compound was prepared from (RS)-[5-morpholin-4-yl-2-(3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-isoxazol-3-yl]-phenyl}-propionylamino)-4-trifluoromethyl-phenyl]-carbamic acid tert.-butyl ester (Example M31) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a white solid (386 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06548495B2
Source datasetuspto-grants-2003_04
ORD IDord-6136225f0c1244ca816955b0e196f60c
Source noteuspto-grants-2003_04