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HRID 13673作成日:2026年10月25日

1-(Methylsulphonyl)acetone → 6-Bromo-3-methanesulfonyl-2-methyl-4-(4-trifluoromethyl-phenyl)-quinoline

https://huagongshe.com/reaction/13673

反応式

関与物質

役割名称HCID仕込み量
反応物1-(Methylsulphonyl)acetoneHCID 78695—
反応物SodiumHCID 5360545—
反応物(2-Amino-5-bromo-phenyl)-(4-trifluoromethyl-phenyl)-methanoneHCID 12001533—
溶媒EthanolHCID 702—
生成物6-Bromo-3-methanesulfonyl-2-methyl-4-(4-trifluoromethyl-phenyl)-quinolineHCID 1200172529.1%

反応手順

(2-Amino-5-bromo-phenyl)-(4-trifluoromethyl-phenyl)-methanone (compound of example A.3) (4 g, 11.6 mmol), methanesulfonylacetone (2.37 g, 17.4 mmol) and sodium tetrachloroaureate(III) dihydrate (0.23 g, 0.58 mmol) were heated at reflux in ethanol (50 ml) for 4 days. The resulting mixture was evaporated to dryness and the residue extracted with dichloromethane (2×), NaOH (2×) and NaCl (1×). The crude product was purified by chromatography on silica gel in heptane/ethyl acetate 70:30. One obtained a light yellow solid (1.5 g, 29%). MS: m/z=444 (M).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07728142B2
出典データセットuspto-grants-2010_06
ORD IDord-7da5d5e5e52a4a668d4398aaa7b5faaa
出典メモuspto-grants-2010_06