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HRID 890407作成日:2026年10月25日

Lithium Hydroxide → HCID 10230069、化合物

https://huagongshe.com/reaction/890407

反応式

関与物質

役割名称HCID仕込み量
反応物Lithium HydroxideHCID 3939—
反応物DiisopropylethylamineHCID 81531—
反応物3-Hydroxypiperidine, (R)-HCID 2759334—
反応物2-[1-(4-(Ethoxycarbonyl)piperazin-1-yl)carbonyl-3-(methoxycarbonyl)propyl]aminocarbonyl-4-chloroquinolineHCID 22017379—
溶媒Dimethyl SulfoxideHCID 679—
生成物HCID 10230069HCID 1023006924.7%

反応条件

温度110 °C

反応手順

To a solution of 2-[1-(4-(ethoxycarbonyl)piperazin-1-yl)carbonyl-3-(methoxycarbonyl)propyl]aminocarbonyl-4-chloroquinoline (150 mg, 0.315 mmol) in DMSO (3.0 mL) was added (R)-3-hydroxypiperidine (68 mg, 0.5 mmol) and DIEA (65 mg, 0.5 mL). The mixture was heated at 110° C. for 18 hours. The crude reaction mixture was treated with lithium hydroxide (3.0 mL 0.25 M) for 4 hours. The reaction was purified by preparative HPLC to afford 2-[1-(4-(ethoxycarbonyl)piperazin-1-yl)carbonyl-3-carboxypropyl]aminocarbonyl-4-(3-hydroxypyrrolidin-1-yl)quinoline (41.0 mg); NMR (DMSO-d6) 1.2 (t, 3), 2.00–2.20 (m, 4), 2.45 (m, 2), 3.30–3.75 (m, 8), 4.05 (q, 2), 4.60 (s, 1), 5.11 (m, 1), 7.39 (s, 1), 7.65 (m, 1), 7.95 (m, 1), 8.28 (m, 1), 8.58 (br s, 1), 9.75 (m, 1) ppm.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06995156B2
出典データセットuspto-grants-2006_02
ORD IDord-333d48e7131d4ce6b051b36ec9c47d9c
出典メモuspto-grants-2006_02