Cesium carbonate → HCID 86685974, compound

Participants

Role	Name	HCID	Charge
Reactant	Cesium carbonate	HCID 10796	—
Reactant	Ethanesulfonamide	HCID 73702	—
Reactant	L-Proline	HCID 145742	—
Reactant	HCID 86685975	HCID 86685975	—
Catalyst	Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)	HCID 24350	—
Solvent	1,4-Dioxane	HCID 31275	—
Product	HCID 86685974	HCID 86685974	20%

Reaction Steps

CuI (1.9 mg, 0.01 mmol), L-proline (2.3 mg, 0.02 mmol) and Cs2CO3 (65 mg, 0.2 mmol) were added to a dioxane (3 mL) solution of 2-(5-bromo-pyridin-3-yl)-6-chloro-3,4-dihydro-2H-isoquinolin-1-one (example 7) (33.7 mg, 0.1 mmol) and ethanesulfonic acid amide (10.9 mg, 0.1 mmol). The resulting reaction mixture was subject to microwave reaction at 150° C. for 2.5 hours. The reaction mixture was filtered and concentrated in vacuo to give a crude product which was then purified by prep-HPLC to give title compound (7.3 mg, 20%) as a white solid. MS: 366.1 (M+H+).

Provenance & Evidence

DOI	10.6084/m9.figshare.5104873.v1
Patent number	US09133158B2
Source dataset	uspto-grants-2015_09
ORD ID	ord-123a1e3e008945df82558a8a8e5ef033
Source note	uspto-grants-2015_09