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HRID 2194138作成日:2026年10月26日

(Trifluoromethyl)trimethylsilane → 8-(2-Chloro-benzenesulfonyl)-2-[4-(2,2,2-trifluoro-1-hydroxy-1-methyl-ethyl)-phenyl]-2,8-diaza-spiro[4.5]decan-1-one

https://huagongshe.com/reaction/2194138

反応式

関与物質

役割名称HCID仕込み量
反応物(Trifluoromethyl)trimethylsilaneHCID 552549—
反応物Tetrabutylammonium FluorideHCID 2724141—
反応物2-(4-Acetyl-phenyl)-8-(2-chloro-benzenesulfonyl)-2,8-diaza-spiro[4.5]decan-1-oneHCID 59577963—
触媒Hydrochloric AcidHCID 313—
溶媒TetrahydrofuranHCID 8028—
生成物8-(2-Chloro-benzenesulfonyl)-2-[4-(2,2,2-trifluoro-1-hydroxy-1-methyl-ethyl)-phenyl]-2,8-diaza-spiro[4.5]decan-1-oneHCID 5957803260.5%

反応手順

2-(4-Acetyl-phenyl)-8-(2-chloro-benzenesulfonyl)-2,8-diaza-spiro[4.5]decan-1-one (0.13 g), product of example 151), dissolved in THF (12 ml) under an argon atmosphere was treated at RT with (trifluoromethyl)trimethylsilane (0.062 g) then with tetra-n-butylammonium fluoride (1M solution in THF, 0.29 ml) and the reaction mixture was stirred overnight at RT. The mixture was made acidic with 3M aqueous HCl (a few drops) and stirred further 15 minutes. The solvent was removed in vacuo and the residue adsorbed on silica gel and chromatographed over silica gel (AcOEt/heptane, gradient from 0 to 40%) to give the desired product as white solid (0.091 g). MS (ESI): 517.1 MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08329904B2
出典データセットuspto-grants-2012_12
ORD IDord-0646c067664e4abd8f11a6ac87460ef8
出典メモuspto-grants-2012_12