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HRID 394614作成日:2026年10月25日

Trifluoroacetic acid → 5'-Chloro-[2,2']bithiophenyl-5-sulfonic acid [2-oxo-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-pyrrolidin-3(S)-yl]-amide

https://huagongshe.com/reaction/394614

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acidHCID 6422—
反応物2-[3-(S)-(5'-Chloro-[2,2']bithiophenyl-5-sulfonylamino)-2-oxo-pyrrolidin-1-ylmethyl]pyrrolo[3,2-c]pyridine-1-carboxylic acid tert-butyl esterHCID 69709209—
生成物5'-Chloro-[2,2']bithiophenyl-5-sulfonic acid [2-oxo-1-(1H-pyrrolo[3,2-c]pyridin-2-ylmethyl)-pyrrolidin-3(S)-yl]-amideHCID 10074410—

反応手順

Trifluoroacetic acid (1.0 mL, 13.0 mmol) is added dropwise to a slurry of 2-[3-(S)-(5′-chloro-[2.2′]bithiophenyl-5-sulfonylamino)-2-oxo-pyrrolidin-1-ylmethyl]pyrrolo[3,2-c]pyridine-1-carboxylic acid tert-butyl ester (0.13 g, 0.22 mmol) in CH2C2 (2 mL) at 0° C. After 30 min the ice bath is removed and the solution is stirred at room temperature for 4 h. The reaction mixture is concentrated to dryness and the crude product is purified by RP-HPLC eluting in a gradient of 10% CH3CN/H2O (0.1% TFA) to 100% CH3CN. The appropriate product fractions are lyophilized to provide the title compound as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06602864B1
出典データセットuspto-grants-2003_08
ORD IDord-ea3b444e17124ebea1a5d7252c315c9c
出典メモuspto-grants-2003_08