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HRID 252242作成日:2026年10月26日

Acetic Acid → N-[(5-bromo-1,3-thiazol-2-yl)carbamoyl]-4-[(3,4-dichloro-1-methyl-1H-pyrazol-5-yl)oxy]benzenesulfonamide

https://huagongshe.com/reaction/252242

反応式

関与物質

役割名称HCID仕込み量
反応物Acetic AcidHCID 176—
反応物1,8-Diazabicyclo(5.4.0)undec-7-eneHCID 81184—
反応物4-(4,5-Dichloro-2-methylpyrazol-3-yl)oxybenzenesulfonamideHCID 1478245—
反応物Diphenyl (5-bromo-1,3-thiazol-2-yl)imidodicarbonateHCID 66858288—
溶媒WaterHCID 962—
溶媒DimethylformamideHCID 6228—
生成物N-[(5-bromo-1,3-thiazol-2-yl)carbamoyl]-4-[(3,4-dichloro-1-methyl-1H-pyrazol-5-yl)oxy]benzenesulfonamideHCID 24780160—

反応手順

4-(4,5-dichloro-2-methyl-2H-pyrazol-3-yloxy)-benzenesulfonamide (77.3 mg, 0.24 mmol) and diphenyl (5-bromo-1,3-thiazol-2-yl)imidodicarbonate (100 mg, 0.24 mmol) were suspended in DMF (0.4 ml). A solution of DBU (0.04 ml, 0.26 mmol) in DMF (0.1 ml) was added dropwise and the clear mixture was shaken for 1.5 h at rt and kept overnight at 4° C. The mixture was acidified using acetic acid (0.2 ml) and diluted with water (0.2 ml) and purified directly using preparative RP(C18)chromatography: lyophilisate 9 mg, MS: m/e 523.8 (MH−).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07868030B2
出典データセットuspto-grants-2011_01
ORD IDord-b834cd58a75a4f18997d8625d3fa8c17
出典メモuspto-grants-2011_01