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HRID 23633作成日:2026年10月24日

Diisopropylethylamine → N-(4-fluorobenzyl)-2-{[[(2R)-2-hydroxy-2-pyrazin-2-ylethyl](methyl)amino]methyl}-3,4-dimethyl-7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamide

https://huagongshe.com/ja/reaction/23633

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物(1R)-2-(methylamino)-1-pyrazin-2-ylethanolHCID 10285809—
反応物N-(4-fluorobenzyl)-2-(chloromethyl)-3,4-dimethyl-7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamideHCID 22574387—
溶媒WaterHCID 962—
溶媒DimethylformamideHCID 6228—
生成物N-(4-fluorobenzyl)-2-{[[(2R)-2-hydroxy-2-pyrazin-2-ylethyl](methyl)amino]methyl}-3,4-dimethyl-7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamideHCID 5998522922.7%

反応手順

A mixture of N-(4-fluorobenzyl)-2-(chloromethyl)-3,4-dimethyl-7-oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamide (104 mg, 0.275 mmol), (1R)-2-(methylamino)-1-pyrazin-2-ylethanol (Preparation 80, 65 mg, 0.0.42 mmol) and diisopropylethylamine (72 μL, 0.0.41 mmol) in dry DMF (5.5 mL) was stirred at room temperature for 17 hours. The solution was then diluted with water (20 mL). The resulting precipitate was collected by filtration and the collected solid was dried in vacuo, providing a white solid. Attempted recrystallization from acetonitrile (20 mL, dissolved with warming and then cooled to room temperature) gave the title compound (31 mg) as a white solid upon concentrating the filtrate.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06852731B2
出典データセットuspto-grants-2005_02
ORD IDord-aee10b747c794fb3bccbcc707476cc3b
出典メモuspto-grants-2005_02