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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1845857Generated: October 31, 2026

4-Bromo-2-fluorobenzeneboronic acid → (R)-(4-(6-Amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-YL)-3-fluorophenyl)dimethylphosphine oxide

https://huagongshe.com/reaction/1845857

Reaction equation

Participants

RoleNameHCIDCharge
Reactant4-Bromo-2-fluorobenzeneboronic acidHCID 2773333—
Reactant(R)-5-bromo-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amineHCID 11689426—
ReactantmethylphosphonoylmethaneHCID 178503022—
SolventIsopropanol hexaneHCID 21585144—
Product(R)-(4-(6-Amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-YL)-3-fluorophenyl)dimethylphosphine oxideHCID 60168720—

Reaction Steps

The title compound was prepared from 5-bromo-3-[(1R)-1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-pyridin-2-ylamine, 4-bromo-2-fluoro-phenylboronic acid, and dimethylphosphine oxide followed the same procedures as Example 1 Step 1 and Step 3; ESMS: m/z 471 (M+H)+; chiral purity 93.12% (column AD-H 4.6*250 mm 5 um; solvent:hexane/isopropanol).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08951993B2
Source datasetuspto-grants-2015_02
ORD IDord-8b4bcbdb2336434fab511bf38242c7e5
Source noteuspto-grants-2015_02