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HRID 30110作成日:2026年10月25日

Triethylamine → [2-Amino-6-(1-ethanesulfonyl-piperidin-4-ylamino)-pyridin-3-yl]-(2-fluoro-phenyl)-methanone

https://huagongshe.com/reaction/30110

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Ethanesulfonyl chlorideHCID 11667—
反応物[2-Amino-6-(piperidin-4-ylamino)-pyridin-3-yl]-(2-fluoro-phenyl)-methanoneHCID 58590835—
溶媒DichloromethaneHCID 6344—
生成物[2-Amino-6-(1-ethanesulfonyl-piperidin-4-ylamino)-pyridin-3-yl]-(2-fluoro-phenyl)-methanoneHCID 1153871760.8%

反応手順

To a solution of [2-Amino-6-(piperidin-4-ylamino)-pyridin-3-yl]-(2-fluoro-phenyl)-methanone (19.2 mg, 0.0611 mmol, Example 9) in methylene chloride (1.5 mL) were added triethylamine (12.6 mg, 0.124 mmol, Aldrich) in methylene chloride (0.2 mL) and a solution of ethanesulfonyl chloride (8.66 mg, 0.066 mmol, Aldrich 99+%) in methylene chloride (0.2 mL) at room temperature. After ˜30 mins the reaction mixture was concentrated and purified by reversed phase HPLC as described in Example 11 to give [2-Amino-6-(1-ethanesulfonyl-piperidin-4-ylamino)-pyridin-3-yl]-(2-fluoro-phenyl)-methanone as a white solid (15.1 mg, 60 % yield). HRMS, observed: 407.1533, calcd for (M+H)+: 407.1548.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07423051B2
出典データセットuspto-grants-2008_09
ORD IDord-8117802aa89c4f1cbc3d4798825a5288
出典メモuspto-grants-2008_09