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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 418545Generated: October 30, 2026

Dichloromethane → 2-(3-Fluoro-4-trifluoromethyl-phenyl)-N-{2-[(R)-2-(3-hydroxy-azetidin-1-yl)-1-methyl-ethyl]-6-methyl-1-oxo-1,2-dihydro-isoquinolin-5-yl}-acetamide

https://huagongshe.com/reaction/418545

Reaction equation

Participants

RoleNameHCIDCharge
ReactantDichloromethaneHCID 6344—
ReactantTriethylamineHCID 8471—
Reactant3-Hydroxyazetidine hydrochlorideHCID 2759290—
Reactant(R)-2-(5-(2-(3-Fluoro-4-(trifluoromethyl)phenyl)acetamido)-6-methyl-1-oxoisoquinolin-2(1H)-yl)propyl methanesulfonateHCID 59845709—
Product2-(3-Fluoro-4-trifluoromethyl-phenyl)-N-{2-[(R)-2-(3-hydroxy-azetidin-1-yl)-1-methyl-ethyl]-6-methyl-1-oxo-1,2-dihydro-isoquinolin-5-yl}-acetamideHCID 25014108—

Reaction Steps

A solution of (R)-2-(5-(2-(3-fluoro-4-(trifluoromethyl)phenyl)acetamido)-6-methyl-1-oxoisoquinolin-2(1H)-yl)propyl methanesulfonate (100 mg, 0.2 mmol), 3-hydroxyazetidine hydrochloride (120 mg, 1.1 mmol), triethylamine (200 mg, 2 mmol) and methylene chloride (1 mL, 20 mmol) was stirred at room temperature overnight. The volatiles were removed and the residue was purified by reverse phase preparative HPLC to afford the desired product as a white solid.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08093265B2
Source datasetuspto-grants-2012_01
ORD IDord-e2eabfc9e354440dabab0d6d4beee60c
Source noteuspto-grants-2012_01