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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 498855Generated: October 31, 2026

Chloride → 4-[3-(2-Methoxymethyl-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/498855

Reaction equation

Participants

RoleNameHCIDCharge
ReactantChlorideHCID 312—
ReactantThionyl ChlorideHCID 24386—
ReactantSodium MethoxideHCID 10942334—
ReactantHCID 22317746HCID 22317746—
SolventMethanolHCID 887—
SolventDichloromethaneHCID 6344—
Product4-[3-(2-Methoxymethyl-pyridin-4-yl)-phenyl]-7-(2,2,2-trifluoro-ethoxy)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-oneHCID 22317935—

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 sodium methanolate (5.4M, 1 ml) in MeOH (5 ml)/CH2Cl2 (5 ml) according to the general procedure of Example 288. Obtained as an off-white solid (94 mg, 36%).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS06949542B2
Source datasetuspto-grants-2005_09
ORD IDord-0998c474a5fa4d3c8bbd586b5962d8e0
Source noteuspto-grants-2005_09