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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 498857Generated: November 1, 2026

Trifluoroacetic acid → 4-(3-(2-(hydroxymethyl)-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-one

https://huagongshe.com/reaction/498857

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant(RS)-[5-Methyl-2-(3-{3-[2-methyl-6-(tetrahydro-pyran-2-yloxymethyl)-pyridin-4-yl]-phenyl}-3-oxo-propionylamino)-4-trifluoromethyl-phenyl]-carbamic acid tert-butyl esterHCID 86589466—
SolventDichloromethaneHCID 6344—
Product4-(3-(2-(hydroxymethyl)-6-methylpyridin-4-yl)phenyl)-7-methyl-8-(trifluoromethyl)-1H-benzo[b][1,4]diazepin-2(3H)-oneHCID 22317918—

Reaction Steps

The title compound was prepared from (RS)-[5-methyl-2-(3-{3-[2-methyl-6-(tetrahydro-pyran-2-yloxymethyl)-pyridin-4-yl]-phenyl}-3-oxo-propionylamino)-4-trifluoromethyl-phenyl]-carbamic acid tert-butyl ester (Example M298) (0.49 g, 0.76 mmol) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a light yellow solid (200 mg, 60%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06949542B2
Source datasetuspto-grants-2005_09
ORD IDord-a3b83c43d47d4db383b7f73b04685a94
Source noteuspto-grants-2005_09