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HRID 74607作成日:2026年10月24日

2-Fluoroisonicotinic acid → 4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4'-carboxylic acid

https://huagongshe.com/ja/reaction/74607

反応式

関与物質

役割名称HCID仕込み量
反応物2-Fluoroisonicotinic acidHCID 345360—
反応物7-methoxy-3-(piperidin-4-yl)-4,5-dihydro-1H-benzo[d][1,3]diazepin-2(3H)-oneHCID 18356852—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-benzo[d][1,3]diazepin-3-yl)-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-4'-carboxylic acidHCID 58386433—

反応手順

6.0 g (22 mmol) 7-methoxy-3-piperidin-4-yl-1,3,4,5-tetrahydro-1,3-benzodiazepin-2-one and 1.5 g (11 mmol) 2-fluoropyridine-4-carboxylic acid in 20 mL NMP were stirred overnight at 110° C. The reaction mixture was cooled and the precipitate formed was suction filtered. This was stirred with water, additionally combined with 15% potassium carbonate solution and extracted several times with DCM. The aqueous phase was acidified, the precipitate formed was suction filtered and dried.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08829006B2
出典データセットuspto-grants-2014_09
ORD IDord-f467d20d7d5e4573954603921c70bfd7
出典メモuspto-grants-2014_09