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HRID 15986作成日:2026年10月27日

Triethylamine → n-(2-(Dimethylamino)ethyl)-n-methyl-4-(3-(quinolin-6-ylmethyl)-3h-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)benzamide

https://huagongshe.com/reaction/15986

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物1,2-Ethanediamine, N1,N1,N2-trimethyl-HCID 67338—
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4-(3-(Quinolin-6-ylmethyl)-3h-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)benzoic acidHCID 59341862—
溶媒DimethylformamideHCID 6228—
生成物n-(2-(Dimethylamino)ethyl)-n-methyl-4-(3-(quinolin-6-ylmethyl)-3h-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)benzamideHCID 4538102157.9%

反応手順

HATU (82 mg, 0.22 mmol) was added to a mixture of 4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)benzoic acid (75 mg, 0.20 mmol), N1,N1,N2-trimethylethane-1,2-diamine (22 mg, 0.22 mmol) and triethylamine (0.060 mL, 0.43 mmol) in DMF (2.0 mL). After stirring for 18 hours, the reaction was partitioned between dichloromethane:ethanol (9:1) and water. The organic layer was separated, dried over Na2SO4, filtered and concentrated by rotary evaporation to afford 108 mg of crude material. The material was purified by pre-HPLC to give N-(2-(dimethylamino)ethyl)-N-methyl-4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)benzamide (54 mg, yield 48%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07732604B2
出典データセットuspto-grants-2010_06
ORD IDord-ca7cbd2bacca4b64818d67886f66b7f8
出典メモuspto-grants-2010_06