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HRID 1845953作成日:2026年10月27日

Triethylamine → (S)-6-{3-(tert-butoxycarbonylamino)pyrrolidin-1-ylsulfonyl}isoquinoline

https://huagongshe.com/reaction/1845953

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物(3S)-(-)-3-(tert-Butoxycarbonylamino)pyrrolidineHCID 1514396—
反応物Isoquinoline-6-sulfonyl chlorideHCID 55280287—
反応物(R)-6-(3-aminopyrrolidin-1-ylsulfonyl)isoquinoline dihydrochlorideHCID 66727170—
溶媒DichloromethaneHCID 6344—
生成物(S)-6-{3-(tert-butoxycarbonylamino)pyrrolidin-1-ylsulfonyl}isoquinolineHCID 66727094—

反応手順

A dichloromethane solution (100 mL) of 6-chlorosulfonylisoquinoline (Reference Compound 2) was added with stirring at room temperature to a solution containing 423 mg of (S)-(−)-3-(tert-butoxycarbonylamino)pyrrolidine dissolved in 20 mL of dichloromethane further supplemented with 0.5 mL of triethylamine, and reacted for 6 hour. The reaction solution was washed with saturated saline and dried over anhydrous sodium sulfate. After filtration, the filtrate was concentrated, and the obtained crude product was purified by silica gel column chromatography (acetone:hexane=1:2) to obtain 560 mg of the compound of interest as a colorless oil (65%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08951997B2
出典データセットuspto-grants-2015_02
ORD IDord-de958c0ddf41474598828c5ca6db4c47
出典メモuspto-grants-2015_02