3,5-Dichlorobenzoic acid → 3,5-dichloro-N-((1-(2-(cyclopropanesulfonamido)ethyl)piperidin-4-yl)methyl)benzamide

関与物質

役割	名称	HCID	仕込み量
反応物	3,5-Dichlorobenzoic acid	HCID 5811	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
反応物	N-(2-(4-(aminomethyl)piperidin-1-yl)ethyl)-1,1,1-trifluoromethanesulfonamide dihydrochloride salt	HCID 67029054	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	3,5-dichloro-N-((1-(2-(cyclopropanesulfonamido)ethyl)piperidin-4-yl)methyl)benzamide	HCID 57993352	—

反応手順

To a solution of 3,5-dichlorobenzoic acid (23 mg, 0.12 mmol) in DMF (2 mL) was added DIPEA (0.1 mL, 0.6 mmol), N-(2-(4-(aminomethyl) piperidin-1-yl)ethyl)-1,1,1-trifluoromethanesulfonamide dihydrochloride salt (40 mg, 0.12 mmol) and HATU (60 mg, 0.15 mmol). The reaction mixture was stirred at room temperature overnight. The organic layer was washed with sat. NaHCO3 aq. (8 mL), dried over Na2SO4, and concentrated to give crude product which was subsequently purified by High Throughput Purification System (HiTOPs).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08377968B2
出典データセット	uspto-grants-2013_02
ORD ID	ord-95ddbb57b44e497b93f652b7f4af4773
出典メモ	uspto-grants-2013_02