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HRID 1432352作成日:2026年10月27日

Diphosgene → 6-(Phenylmethyl)-1,6-diazabicyclo[3,2,1]octan-7-one

https://huagongshe.com/reaction/1432352

反応式

関与物質

役割名称HCID仕込み量
反応物DiphosgeneHCID 10426—
反応物N-benzylpiperidin-3-amineHCID 21942046—
溶媒TolueneHCID 1140—
生成物6-(Phenylmethyl)-1,6-diazabicyclo[3,2,1]octan-7-oneHCID 2194215330%

反応条件

温度0 °C

反応手順

1.06 g of product obtained in Stage C is dissolved in 28 cm3 of toluene, then the reaction medium is cooled down to 0° C. and 337 μl of diphosgene is added under an inert gas. The temperature is allowed to rise and is maintained at 20° C. for 2 hours. Concentration is carried out under reduced pressure then the residue is chromatographed on silica eluting successively with methylene chloride-acetone 95/5 then 80/20 and finally methylene chloride-methanol, triethylamine 92/8/3 and 362 mg of expected product C13H16N2O (M=216.85 g) is obtained i.e. a yield of 30%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07612087B2
出典データセットuspto-grants-2009_11
ORD IDord-a8f02fa77a704f61956f37fdc27aaac2
出典メモuspto-grants-2009_11