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HRID 536321作成日:2026年10月24日

Pyridine → Cyclopropanesulfonic acid [2-methyl-6-((2S,3'R)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-pyridin-3-yl]-amide

https://huagongshe.com/ja/reaction/536321

反応式

関与物質

役割名称HCID仕込み量
反応物PyridineHCID 1049—
反応物Tris(hydroxymethyl)aminomethaneHCID 6503—
反応物Cyclopropanesulfonyl chlorideHCID 2760919—
反応物2-methyl-6-[(3R)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-amineHCID 67480461—
溶媒1,2-DichloroethaneHCID 11—
生成物Cyclopropanesulfonic acid [2-methyl-6-((2S,3'R)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-pyridin-3-yl]-amideHCID 5459715829.6%

反応手順

To a solution of 2-methyl-6-[(3R)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-amine (22.7 mg, 0.09 mmol) in DCE (1 mL) was added pyridine (0.22 mL, 2.7 mmol) followed by a solution of cyclopropanesulfonyl chloride (38 mg, 0.27 mmol) in DCE (1 mL) and stirred at ambient temperature for 5 hours. To this mixture was then added trisamine resin (200 mg, 0.8 mmol, 4 mmol/g loading), stirred for 30 min, filtered and concentrated to afford a crude solid which was purified by flash column chromatography (5% 7N NH3 in MeOH/CH2Cl2) to obtain 9.7 mg of the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08859588B2
出典データセットuspto-grants-2014_10
ORD IDord-97027eb5b6f64f58b71ad1f0c0dae2ad
出典メモuspto-grants-2014_10