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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 498836Generated: November 1, 2026

Chloride → 4-[3-(2-Pyrrolidin-1-ylmethyl-pyridin-4-yl)-phenyl]-7-(2,2,2-trifluoro-ethoxy)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

https://huagongshe.com/reaction/498836

Reaction equation

Participants

RoleNameHCIDCharge
ReactantChlorideHCID 312—
ReactantThionyl ChlorideHCID 24386—
ReactantPyrrolidineHCID 31268—
ReactantHCID 22317746HCID 22317746—
SolventDimethylformamideHCID 6228—
SolventDichloromethaneHCID 6344—
Product4-[3-(2-Pyrrolidin-1-ylmethyl-pyridin-4-yl)-phenyl]-7-(2,2,2-trifluoro-ethoxy)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 22317344—

Reaction Steps

The title compound was prepared from 4-[3-(2-hydroxymethyl-pyridin-4-yl)-phenyl]-7-(2,2,2-trifluoro-ethoxy)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one (Example 286) (255 mg, 0.50 mmol) by reaction with thionylchloride in CH2Cl2 and subsequent treatment of the corresponding crude chloride with pyrrolidine in DMF according to the general procedure of example 288. Obtained as a light brown solid (225 mg, 80%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06949542B2
Source datasetuspto-grants-2005_09
ORD IDord-feec0e96bab34eaf8d51c5ad2d12c321
Source noteuspto-grants-2005_09