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HRID 561379作成日:2026年10月26日

2,2-Dimethyl-1,3-dioxane-4,6-dione → 5-[(4-Chloro-2-fluorophenyl){7-[(methylsulfanyl)methyl]-1H-indol-3-yl}methyl]-2,2-dimethyl-1,3-dioxane-4,6-dione

https://huagongshe.com/reaction/561379

反応式

関与物質

役割名称HCID仕込み量
反応物2,2-Dimethyl-1,3-dioxane-4,6-dioneHCID 16249—
反応物4-Chloro-2-fluorobenzaldehydeHCID 2724908—
反応物7-[(Methylsulfanyl)methyl]-1H-indoleHCID 58392187—
触媒proline dl-formHCID 614—
溶媒AcetonitrileHCID 6342—
生成物5-[(4-Chloro-2-fluorophenyl){7-[(methylsulfanyl)methyl]-1H-indol-3-yl}methyl]-2,2-dimethyl-1,3-dioxane-4,6-dioneHCID 5839247392.1%

反応手順

1.48 g (9.31 mmol) of 4-chloro-2-fluorobenzaldehyde, 1.34 g (9.31 mmol) of Meldrum's acid and 48.7 mg (0.42 mmol) of D,L-proline were added to a solution of 1.50 g (8.46 mmol) of the compound from Example 8A in 70 ml of acetonitrile. The reaction mixture was stirred at RT overnight. It was concentrated, and the residue was taken up in ethyl acetate, washed with saturated aqueous sodium bicarbonate solution, water and saturated aqueous sodium chloride solution, dried over magnesium sulfate, filtered and concentrated. 3.60 g of the title compound were obtained and were reacted without further purification.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08063234B2
出典データセットuspto-grants-2011_11
ORD IDord-7be1da5f4545427aa7deb9bcf8b38c60
出典メモuspto-grants-2011_11