1-Hydroxybenzotriazole → (2(S)-Pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-(4-thiophen-2-yl-phenyl)-methanone

참여 물질

역할	이름	HCID	투입량
반응물	1-Hydroxybenzotriazole	HCID 75771	—
반응물	Diisopropylethylamine	HCID 81531	—
반응물	4-(Thiophen-2-yl)benzoic acid	HCID 736498	—
반응물	(S)-(+)-1-(2-Pyrrolidinylmethyl)pyrrolidine	HCID 853152	—
반응물	1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride	HCID 2723939	—
용매	dichloromethane N,N-dimethylformamide	HCID 22350042	—
생성물	(2(S)-Pyrrolidin-1-ylmethyl-pyrrolidin-1-yl)-(4-thiophen-2-yl-phenyl)-methanone	HCID 11493848	35%

반응 단계

The title compound is prepared in a manner substantially analogous to General Procedure D in 10 mL 10% DMF/dichloromethane using 4-(thiophen-2-yl)-benzoic acid (CAS 29886-62-2) (182 mg, 0.89 mmol), EDC-HCl (254 mg, 1.33 mmol), HOBt (180 mg, 1.33 mmol), DIEA (0.39 mL, 2.22 mmol) and (S)(+)-1-(2-pyrrolidinylmethyl)pyrrolidine (116 mg, 10.0 mmol) to give the title compound (90 mg, 35% yield). MS (ES+) 341.2 (M+H)+

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US07705025B2
출처 데이터셋	uspto-grants-2010_04
ORD ID	ord-412dbde9c74e4402a52a25f6dc0f6adc
출처 메모	uspto-grants-2010_04