Cesium carbonate → 4-[2-(5-Chloro-2-fluoro-phenyl)-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidin-4-ylamino]-nicotinic acid methyl ester

참여 물질

역할	이름	HCID	투입량
반응물	Cesium carbonate	HCID 10796	—
반응물	Methyl 4-aminopyridine-3-carboxylate	HCID 592353	—
반응물	Binap, (A+-)-	HCID 634876	—
반응물	2-(5-Chloro-2-fluoro-phenyl)-4-iodo-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidine	HCID 21104309	—
촉매	palladium(II) acetate	HCID 167845	—
용매	1,4-Dioxane	HCID 31275	—
생성물	4-[2-(5-Chloro-2-fluoro-phenyl)-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidin-4-ylamino]-nicotinic acid methyl ester	HCID 58866042	34%

반응 조건

온도	85 °C

반응 단계

To a solution of 2-(5-Chloro-2-fluoro-phenyl)-4-iodo-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidine (500 mg, 1.24 mmol), 4-amino-nicotinic acid methyl ester (208 mg, 1.37 mmol), Pd(OAc)2 (14 mg, 62.09 μmol) and Rac-BINAP (60 mg, 93.14 μmol) in dry dioxane (10 mL) was added Cs2CO3 (607 mg, 1.86 mmol). The mixture was heated for 12 h at 85° C., cooled and evaporated. The residue was purified by chromatography (CH2Cl2, 0-10% MeOH) to give the desired product (178 mg, 34% yield).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US07977342B2
출처 데이터셋	uspto-grants-2011_07
ORD ID	ord-040016ec6429455caa5df4c81638b485
출처 메모	uspto-grants-2011_07