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HRID 1994758作成日:2026年10月25日

Dimethylformamide → N-methyl-N-(2-{5-[(2-oxo-1-oxa-3,8-diazaspiro[4.5]dec-8-yl)methyl]-1,3-thiazol-2-yl}-1H-indol-7-yl)thiophene-2-sulfonamide

https://huagongshe.com/reaction/1994758

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylformamideHCID 6228—
反応物TriethylamineHCID 8471—
反応物1-Oxa-3,8-diazaspiro(4.5)decan 2-oneHCID 12954114—
反応物N-{2-[5-(chloromethyl)-1,3-thiazol-2-yl]-1H-indol-7-yl}-N-methylthiophene-2-sulfonamideHCID 57475969—
溶媒WaterHCID 962—
生成物N-methyl-N-(2-{5-[(2-oxo-1-oxa-3,8-diazaspiro[4.5]dec-8-yl)methyl]-1,3-thiazol-2-yl}-1H-indol-7-yl)thiophene-2-sulfonamideHCID 5913612543%

反応手順

A mixture of N-{2-[5-(chloromethyl)-1,3-thiazol-2-yl]-1H-indol-7-yl}-N-methylthiophene-2-sulfonamide (150 mg), triethylamine (150 μL), 1-oxa-3,8-diazaspiro[4.5]decan-2-one (110 mg) and N,N-dimethylformamide (2 ml) was stirred at room temperature for 3 hr. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The ethyl acetate layer was washed with saturated brine, dried (MgSO4), and concentrated. The obtained residue was subjected to silica gel column chromatography to give the title compound (82 mg, yield 43%) as colorless crystals from a fraction eluted with ethyl acetate. melting point 224° C.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07652133B2
出典データセットuspto-grants-2010_01
ORD IDord-124b652828014b7dac8bb8e567e24c98
出典メモuspto-grants-2010_01