Ammonia → tert-butyl 4-[(2S)-3-amino-2-hydroxy-propyl]piperazine-1-carboxylate

HRID 2364687ノート

反応式

HRID 2364687 の反応式
[O:1]1[CH2:3][C@H:2]1[CH2:4][N:5]1[CH2:10][CH2:9][N:8]([C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])[CH2:7][CH2:6]1.[NH3:18]>C(O)C>[NH2:18][CH2:3][C@H:2]([OH:1])[CH2:4][N:5]1[CH2:10][CH2:9][N:8]([C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])[CH2:7][CH2:6]1

参加物

4

反応物 2

HCID 222AmmoniaHCID 11010131Tert-butyl 4-[[(2R)-oxiran-2-yl]methyl]piperazine-1-carboxylate

生成物 1

HCID 7144880tert-butyl 4-[(2S)-3-amino-2-hydroxy-propyl]piperazine-1-carboxylate

試薬・触媒・溶媒 1

HCID 702Ethanol溶媒

反応条件

温度
50 °C

実験手順

Tert-butyl 4-[[(2R)-oxiran-2-yl]methyl]piperazine-1-carboxylate 7b (3.55 g, 14.70 mmol) was dissolved in 40 mL of ethanol followed by the addition of 40 mL of aqueous ammonia, stirred for 12 hours. The resulting solution was heated to 50° C. and stirred for another 1 hour, then concentrated under reduced pressure to obtain the crude title compound tert-butyl 4-[(2S)-3-amino-2-hydroxy-propyl]piperazine-1-carboxylate 7c (3.40 g) as a light yellow solid, which was used in the next step without further furification.

後処理

  1. stirringstirred for another 1 hour
  2. concentrationconcentrated under reduced pressure

出典と根拠

ORDレコード
ord-a6815d09190c420f9a36eab9d568d9cb
出典データセット
uspto-grants-2014_04
特許番号
US08691822B2

反応ノート

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