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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1259381Generated: November 1, 2026

Boron Trichloride → 3-Hydroxy-cyclobutanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-1,2,3,5-tetrahydro-imidazo[1,2-a]pyridin-8-yl]-amide

https://huagongshe.com/reaction/1259381

Reaction equation

Participants

RoleNameHCIDCharge
ReactantBoron TrichlorideHCID 25135—
Reactant3-Benzyloxy-cyclobutanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-1,2,3,5-tetrahydro-imidazo[1,2-a]pyridin-8-yl]-amideHCID 67194298—
SolventDichloromethaneHCID 6344—
Product3-Hydroxy-cyclobutanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-1,2,3,5-tetrahydro-imidazo[1,2-a]pyridin-8-yl]-amideHCID 5293501729.5%

Reaction Steps

3-Benzyloxy-cyclobutanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-1,2,3,5-tetrahydro-imidazo[1,2-a]pyridin-8-yl]-amide (120 mg, 0.19 mmol) in DCM (3 mL) was reacted with 1M BCl3 (67 mg, 0.57 mmol) at 0° C. The resulting mixture was stirred at room temperature for 6 hours. Purification by column chromatography on silica gel (5% MeOH in CHCl3), followed by preparative HPLC afforded 30 mg of the product (29.4% yield).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08466289B2
Source datasetuspto-grants-2013_06
ORD IDord-887374bc665f4692b1a6e640c8041d85
Source noteuspto-grants-2013_06