Dichloromethane → 2-(6-Chloro-5-(2-(4-fluoro-3-(trifluoromethyl)phenyl)acetamido)-1-oxoisoquinolin-2(1H)-yl)ethyl acetate

Beteiligte Stoffe

Rolle	Name	HCID	Einwaage
Edukt	Dichloromethane	HCID 6344	—
Edukt	Diisopropylethylamine	HCID 81531	—
Edukt	4-Fluoro-3-(trifluoromethyl)phenylacetic acid	HCID 2737593	—
Edukt	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
Edukt	2-(5-Amino-6-chloro-1-oxoisoquinolin-2(1H)-yl)ethyl acetate	HCID 59515676	—
Produkt	2-(6-Chloro-5-(2-(4-fluoro-3-(trifluoromethyl)phenyl)acetamido)-1-oxoisoquinolin-2(1H)-yl)ethyl acetate	HCID 59515871	—

Reaktionsbedingungen

Temperatur	45 °C

Reaktionsschritte

A reaction vial was charged with 2-(5-amino-6-chloro-1-oxoisoquinolin-2(1H)-yl)ethyl acetate (60.0 mg, 0.000214 mol), 2-(4-fluoro-3-(trifluoromethyl)phenyl)acetic acid (57.0 mg, 0.000256 mol), N,N,N′,N′-tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (203 mg, 0.000534 mol), N,N-diisopropylethylamine (0.093 mL, 0.00053 mol) and methylene chloride (3 mL, 0.05 mol), and the reaction mixture was stirred at 45° C. for 4 days. The solvent was removed under reduced pressure and the residue was purified by flash chromatography to afford the product as a light yellow solid.

Herkunft & Nachweise

DOI	10.6084/m9.figshare.5104873.v1
Patentnummer	US08093265B2
Quelldatensatz	uspto-grants-2012_01
ORD ID	ord-494ad3b39a3547508fe10bdd3f706062
Quellennotiz	uspto-grants-2012_01