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HRID 2196093作成日:2026年10月27日

2,3-Dihydroxy-4-methoxybenzoic acid → 7-Methoxy-1'-acetyl-spiro[1,3-benzodioxole-2,4'-piperidine]-4-carboxylic acid

https://huagongshe.com/reaction/2196093

反応式

関与物質

役割名称HCID仕込み量
反応物2,3-Dihydroxy-4-methoxybenzoic acidHCID 77534—
反応物1-Acetyl-4,4-dimethoxy-piperidineHCID 12653646—
反応物1-Acetyl-4-methoxy-1,2,3,6-tetrahydropyridineHCID 18799218—
生成物7-Methoxy-1'-acetyl-spiro[1,3-benzodioxole-2,4'-piperidine]-4-carboxylic acidHCID 5928672726.3%

反応条件

温度180 °C

反応手順

A mixture of 2,3-dihydroxy-4-methoxybenzoic acid (1.23 g, 6.67 mmol), 1-acetyl-4,4-dimethoxy-piperidine (1.4 g, 7.6 mmol) and 1-acetyl-1,2,3,6-tetrahydro-4-methoxy-pyridine (14.2 g, 91.5 mmol) was exposed to microwave heating (180° C., one hour) in a sealed reaction vessel. Filtration and subsequent standard HPLC purification afforded compound 508 (0.54 g, 26%). LC/MS (METHOD B): (m/z) 308.2 (MH+); RT=2.27 min; purity (UV)=95%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08338431B2
出典データセットuspto-grants-2012_12
ORD IDord-e9fd4a743a404e43a1011bb7e10de4ca
出典メモuspto-grants-2012_12