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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 498755Generated: October 31, 2026

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

https://huagongshe.com/reaction/498755

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
ReactantHCID 86589438HCID 86589438—
SolventDichloromethaneHCID 6344—
Product8-Chloro-4-[3-(2-hydroxymethyl-pyridin-4-yl)-phenyl]-7-methyl-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 22317726—

Reaction Steps

The title compound was prepared from (RS)-[4-chloro-5-methyl-2-(3-oxo-3-{3-[2-(tetrahydro-pyran-2-yloxymethyl)-pyridin-4-yl]-phenyl}-propionylamino)-phenyl]-carbamic acid tert-butyl ester (Example M259) (0.50 g, 0.84 mmol) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as an off-white solid (182 mg, 55%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06949542B2
Source datasetuspto-grants-2005_09
ORD IDord-d7c003f995484340bcee11adc38d3358
Source noteuspto-grants-2005_09