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HRID 29777作成日:2026年10月27日

Pyridine → 1-{4-[(5,5-Dioxido-2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazin-7-yl)oxy]phenyl}ethanone

https://huagongshe.com/reaction/29777

反応式

関与物質

役割名称HCID仕込み量
反応物PyridineHCID 1049—
反応物4-Acetylphenylboronic acidHCID 3702122—
反応物2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazin-7-ol 5,5-dioxideHCID 9813518—
触媒Cupric acetateHCID 8895—
溶媒DichloromethaneHCID 6344—
生成物1-{4-[(5,5-Dioxido-2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c][1,2,4]benzothiadiazin-7-yl)oxy]phenyl}ethanoneHCID 69200065—

反応手順

A suspension composed of 3.0 g (12.48 mmol) of 2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c]-[1,2,4]benzothiadiazin-7-ol 5,5-dioxide, 3.18 g (18.73 mmol) of (4-acetylphenyl)boronic acid, 3.42 g (18.82 mmol) of copper(II) acetate, 3.03 ml (37.15 mmol) of pyridine and about 500 mg of 4 Å molecular sieve in 150 ml of methylene chloride is stirred overnight. The reaction mixture is diluted by adding a further 100 ml of methylene chloride and the suspension is filtered. The filtrate is concentrated and then directly placed on a silica column which is eluted with a CH2Cl2/acetone 99/1 system. The fractions containing the expected product are combined and evaporated, and the residue is taken up in ethyl ether. After filtering off the solid, the title product is recovered in the form of white powder.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07423034B2
出典データセットuspto-grants-2008_09
ORD IDord-7daf83d4729544bdadb3b45540297135
出典メモuspto-grants-2008_09