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HRID 732作成日:2026年10月23日

2-Bromopyridine → (4-Cyclobutyl-piperazin-1-yl)-(6-pyridin-2-yl-6-aza-spiro[2.5]oct-1-yl)-methanone

https://huagongshe.com/ja/reaction/732

反応式

関与物質

役割名称HCID仕込み量
反応物2-BromopyridineHCID 7973—
反応物(6-Aza-spiro[2.5]oct-1-yl)-(4-cyclobutyl-piperazin-1-yl)-methanoneHCID 59395236—
試薬Sodium t-butoxideHCID 23676156—
触媒Palladium (II) acetateHCID 4144353—
触媒2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenylHCID 11155794—
生成物(4-Cyclobutyl-piperazin-1-yl)-(6-pyridin-2-yl-6-aza-spiro[2.5]oct-1-yl)-methanoneHCID 251195439.39%

反応条件

温度160 °C

反応手順

Reagents were put in a sealed vial and heated in the microwave oven for 10 minutes at 160°C. According to LC-MS analysis, the conversion is >90%. The crude mixture was transferred to a round-bottomed flask and volatiles were evaporated under vacuum. The residue was purified on preparative HPLC using the long high pH (acetonitrile in water ammonium carbonate buffer, 25 min.) 20 to 40% gradient method on XBridge Prep C18 OBD, 30x150 mm, 5 mm, Waters reverse phase column, giving (4-cyclobutylpiperazin-1-yl)(6-(pyridin-2-yl)-6-azaspiro[2.5]octan-1-yl)methanone (7.20 mg, 9.39 %). However, the compound was not pure enought for submission and there was not enough of it to attempt another purification.

情報源と証拠

出典データセット750 AstraZeneca ELN dataset
ORD IDord-c35b162a34bf408282b33e4af9af7634
出典メモ750 AstraZeneca ELN dataset