2-Ethoxy-1-naphthoic acid → 2-[(2-Ethoxy-naphthalene-1-carbonyl)-amino]-indan-2-carboxylic acid ethyl ester

참여 물질

역할	이름	HCID	투입량
반응물	2-Ethoxy-1-naphthoic acid	HCID 75210	—
반응물	Diisopropylethylamine	HCID 81531	—
반응물	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
반응물	Ethyl 2-amino-2,3-dihydro-1H-indene-2-carboxylate	HCID 10921653	—
용매	Dimethylformamide	HCID 6228	—
생성물	2-[(2-Ethoxy-naphthalene-1-carbonyl)-amino]-indan-2-carboxylic acid ethyl ester	HCID 59314345	67.2%

반응 단계

To a solution of 2-ethoxy-naphthalene-1-carboxylic acid (335 mg, 1.55 mmol), 2-amino-indan-2-carboxylic acid ethyl ester (318 mg, 1.55 mmol), HATU (886 mg, 2.33 mmol) in anhydrous DMF (8 mL) is added DIPEA (385 μL, 2.33 mmol). The resulting solution is stirred at RT overnight. After the removal of DMF in vacuo, the residue is dissolved in EtOAc (40 mL) and washed with water (1×10 mL) and brine (2×10 mL). The organic layer is dried over anhydrous Na2SO4 and concentrated in vacuo. The residue is purified by flash column chromatography (115 g silica gel, gradient elution: 5-50% EtOAc in heptane) to give a pure product (45) as white solid (420 mg, 67%).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08569535B2
출처 데이터셋	uspto-grants-2013_10
ORD ID	ord-a81bf9229bd542ff910d79010f6664e5
출처 메모	uspto-grants-2013_10