Triethylamine → 2-[4-Methoxy-3-(4-trifluoromethyl-phenylethynyl)-benzoylamino]-indane-2-carboxylic acid methyl ester

참여 물질

역할	이름	HCID	투입량
반응물	Triethylamine	HCID 8471	—
반응물	1-Ethynyl-4-(trifluoromethyl)benzene	HCID 4348295	—
반응물	2-(3-Bromo-4-methoxy-benzoylamino)-indane-2-carboxylic acid methyl ester	HCID 67076330	—
촉매	Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)	HCID 24350	—
촉매	HCID 178418397	HCID 178418397	—
용매	Toluene	HCID 1140	—
생성물	2-[4-Methoxy-3-(4-trifluoromethyl-phenylethynyl)-benzoylamino]-indane-2-carboxylic acid methyl ester	HCID 67076275	11%

반응 조건

온도	100 °C

반응 단계

300 mg (0.74 mmol) of the compound of step 1 and 90.1 mg (0.89 mmol) of triethylamine were dissolved in 10 ml of dry toluene. 171.5 mg (148 μmol) of tetrakis(triphenylphosphine)palladium(0) and 14.1 mg (74 μmol) of copper(I) iodide were added, and the mixture was stirred for 30 min. Subsequently 126.2 mg (0.74 mmol) of 1-ethynyl-4-trifluoromethyl-benzene were added and the mixture was heated to 100° C. for 10 h. The mixture was filtered, the solvent was evaporated and the residue was purified by preparative RP HPLC (water/ACN gradient) to give 40 mg of the title compound.

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US09328071B2
출처 데이터셋	uspto-grants-2016_05
ORD ID	ord-c639e0fb28d94a22b7ae165c5527fb21
출처 메모	uspto-grants-2016_05