Hydrochloric Acid → (2E)-3-[5-({(3R)-1-[2-(dimethylamino) benzyl]-3-pyrrolidinyl}amino)-2-pyrazinyl]acrylic acid
反応式
[CH3:1][N:2]([CH3:28])[C:3]1[CH:27]=[CH:26][CH:25]=[CH:24][C:4]=1[CH2:5][N:6]1[CH2:10][CH2:9][C@@H:8]([NH:11][C:12]2[N:13]=[CH:14][C:15](/[CH:18]=[CH:19]/[C:20]([O:22]C)=[O:21])=[N:16][CH:17]=2)[CH2:7]1.[OH-].[Na+].Cl>CO>[CH3:28][N:2]([CH3:1])[C:3]1[CH:27]=[CH:26][CH:25]=[CH:24][C:4]=1[CH2:5][N:6]1[CH2:10][CH2:9][C@@H:8]([NH:11][C:12]2[N:13]=[CH:14][C:15](/[CH:18]=[CH:19]/[C:20]([OH:22])=[O:21])=[N:16][CH:17]=2)[CH2:7]1参加物
5
反応物 3
生成物 1
試薬・触媒・溶媒 1
反応条件
- 温度
- 55 °C
実験手順
To a solution of methyl (2E)-3-[5-({(3R)-1-[2-(dimethylamino) benzyl]-3-pyrrolidinyl}amino)-2-pyrazinyl]acrylate (235 mg) in MeOH (1.9 mL) was added 1N NaOH aq. (1.2 mL), which was stirred at 55° C. for 1 hour. To the reaction mixture was added 1N—HCl aq. (1.2 mL), and evaporated in vacuo to give a crude (2E)-3-[5-({(3R)-1-[2-(dimethylamino)benzyl]-3-pyrrolidinyl}amino)-2-pyrazinyl]acrylic acid as, a brown solid (0.310 mg). This was used next reaction without purification.
後処理
- customevaporated in vacuo
出典と根拠
- ORDレコード
- ord-0cd47b884fa8490099b9663803b4e17e
- 出典データセット
- uspto-grants-2010_07
- 特許番号
- US07750155B2
反応ノート
読み込み中…