Potassium Carbonate → (R)-2-(4-cyano-3-(5-methylisoxazol-3-ylamino)phenylamino)-4-methylpentanamide

참여 물질

역할	이름	HCID	투입량
반응물	Potassium Carbonate	HCID 11430	—
반응물	3-Amino-5-methylisoxazole	HCID 66172	—
반응물	Binap, (A+-)-	HCID 634876	—
반응물	(R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamide	HCID 67509372	—
촉매	palladium(II) acetate	HCID 167845	—
용매	1,4-Dioxane	HCID 31275	—
생성물	(R)-2-(4-cyano-3-(5-methylisoxazol-3-ylamino)phenylamino)-4-methylpentanamide	HCID 67510964	19.7%

반응 단계

A mixture of (R)-2-(3-bromo-4-cyanophenylamino)-4-methylpentanamide (120 mg, 0.387 mmol), 3-amino-5-methylisoxazole (60 mg, 0.612 mmol), BINAP (40 mg, 0.064 mmol), Pd(OAc)2 (30 mg, 0.13 mmol) and K2CO3 (150 mg, 1.08 mmol) in dioxane (3 mL) was degassed with Ar, then was stirred at 120 C for 18 h. The mixture was concentrated in vacuo. The residue was purified by HPLC to give (R)-2-(4-cyano-3-(5-methylisoxazol-3-ylamino)phenylamino)-4-methylpentanamide (25 mg).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08846928B2
출처 데이터셋	uspto-grants-2014_09
ORD ID	ord-564a0593e8774134aa927e1dae04c80e
출처 메모	uspto-grants-2014_09