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HRID 1181844作成日:2026年10月25日

Piperidine → 2-[(5-chloro-1H-indol-3-yl)methyl]-7-isobutyl-5-methyl-3-(3-methylisoxazol-4yl)-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione

https://huagongshe.com/reaction/1181844

反応式

関与物質

役割名称HCID仕込み量
反応物PiperidineHCID 8082—
反応物IsoxazoleHCID 9254—
反応物1,2-Oxazole-3-carbaldehydeHCID 18373078—
反応物5-chloro-1H-indole-3-carbaldehyde (3-isobutyl-1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)hydrazoneHCID 136334112—
溶媒WaterHCID 962—
溶媒DimethylformamideHCID 6228—
溶媒Ethyl AcetateHCID 8857—
生成物2-[(5-chloro-1H-indol-3-yl)methyl]-7-isobutyl-5-methyl-3-(3-methylisoxazol-4yl)-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dioneHCID 58981055—

反応手順

5-Chloro-1H-indole-3-carbaldehyde(3-isobutyl-1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)hydrazone (100 mg) was added to a solution of isoxazolaldehyde (86 mg) in dimethylformamide at RT. Piperidine (100 uL) was then added and brought to 80 C for 8 h. After cooling to RT, ethyl acetate (25 mL) was added to brown solution and water (25 mL) was added and extracted. The aqueous layer was back extract with ethyl acetate and then combined. The organic layer was dried over sodium sulfate, filtered and removal of solvent to give an amorphous solid. The isoxazole was submitted the Gilson Preparatory chromatography to give a 100 mg of white solids. ES M+H+467.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07285558B2
出典データセットuspto-grants-2007_10
ORD IDord-e70ab77086a047909137d39918ee7684
出典メモuspto-grants-2007_10