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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 498738Generated: October 26, 2026

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

https://huagongshe.com/reaction/498738

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant[2-{3-[3-(2-Methyl-pyridin-4-yl)-phenyl]-3-oxo-propionylamino}-5-(tetrahydro-pyran-2-yloxymethyl)-4-trifluoromethyl-phenyl]-carbamic acid tert-butyl esterHCID 86589425—
SolventDichloromethaneHCID 6344—
Product7-Hydroxymethyl-4-[3-(2-methyl-pyridin-4-yl)-phenyl]-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 22317716—

Reaction Steps

The title compound was prepared from [2-{3-[3-(2-methyl-pyridin-4-yl)-phenyl]-3-oxo-propionylamino}-5-(tetrahydro-pyran-2-yloxymethyl)-4-trifluoromethyl-phenyl]-carbamic acid tert-butyl ester (Example M241) (156 mg, 0.28 mmol) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a light yellow solid (50 mg, 42%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06949542B2
Source datasetuspto-grants-2005_09
ORD IDord-b08d24a1f8714d0090bc90eab820bf89
Source noteuspto-grants-2005_09