Benzoic Acid → benzyl (3R)-4-(5-cyano-2-iodophenoxy)-3-[4-(pyrrolidine-1-carbonyl)benzoylamino]butyrate
反応式
[Cl-].[CH2:2]([O:9][C:10]([CH2:12][C@@H:13]([NH3+:25])[CH2:14][O:15][C:16]1[CH:21]=[C:20]([C:22]#[N:23])[CH:19]=[CH:18][C:17]=1[I:24])=[O:11])[C:3]1[CH:8]=[CH:7][CH:6]=[CH:5][CH:4]=1.[C:26](O)(=[O:33])[C:27]1[CH:32]=[CH:31]C=[CH:29][CH:28]=1.[OH:35]N1C2C=CC=CC=2N=N1.[CH2:45]([N:47]([CH2:50][CH3:51])[CH2:48][CH3:49])[CH3:46].Cl.CN(C)CCCN=C=NCC>ClCCl.O>[C:22]([C:20]1[CH:19]=[CH:18][C:17]([I:24])=[C:16]([CH:21]=1)[O:15][CH2:14][C@H:13]([NH:25][C:26](=[O:33])[C:27]1[CH:32]=[CH:31][C:46]([C:45]([N:47]2[CH2:50][CH2:51][CH2:49][CH2:48]2)=[O:35])=[CH:29][CH:28]=1)[CH2:12][C:10]([O:9][CH2:2][C:3]1[CH:4]=[CH:5][CH:6]=[CH:7][CH:8]=1)=[O:11])#[N:23]参加物
8
反応物 5
生成物 1
試薬・触媒・溶媒 2
実験手順
2.0 g (4.23 mmol) of (1R)-1-benzyloxycarbonylmethyl-2-(5-cyano-2-iodophenoxy)ethyl ammonium chloride, 1.02 g (4.65 mmol) of 4-pyrrolidine-1-carbonyl)benzoic acid, 630 mg (4.65 mmol) of 1-hydroxybenzotriazole, and 1.30 ml (9.31 mmol) of triethylamine were dissolved in 40 ml of dichloromethane, and 890 mg (4.65 mmol) of 1-(3-dimethylaminopropyl)-3-ethyl carbodiimide hydrochloride was added thereto and stirred under cooling with ice for 10 minutes and then at room temperature for 18 hours. The reaction was stopped by adding water, and the title compound was obtained in an ordinary manner by treatment with dichloromethane as the extractant.
後処理
- temperatureunder cooling with ice for 10 minutes
出典と根拠
- ORDレコード
- ord-668648b39abc4945a20eb03e2dccf5a3
- 出典データセット
- uspto-grants-2008_07
- 特許番号
- US07396844B1
反応ノート
読み込み中…