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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1265792Generated: October 30, 2026

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

https://huagongshe.com/reaction/1265792

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant(RS)-[4-Chloro-5-dimethylamino-2-(3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-isoxazol-3-yl]-phenyl}-propionylamino)-phenyl]-carbamic acid tert.-butyl esterHCID 86586836—
SolventDichloromethaneHCID 6344—
Product8-Chloro-7-dimethylamino-4-[3-(5-hydroxymethyl-isoxazol-3-yl)-phenyl]-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 18613471—

Reaction Steps

The title compound was prepared from (RS)-[4-chloro-5-dimethylamino-2-(3-oxo-3-{3-(5-(tetrahydro-pyran-2-yloxymethyl)-isoxazol-3-yl]-phenyl}-propionylamino)-phenyl]-carbamic acid tert.-butyl ester (Example M43) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a yellow solid (113 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06544985B2
Source datasetuspto-grants-2003_04
ORD IDord-19cd562becc042fcae40cb9221945177
Source noteuspto-grants-2003_04