1,2-Dichloroethane → HCID 57889973、化合物

HRID 1016197ノート

反応式

HRID 1016197 の反応式
[CH3:1][CH:2]([CH3:14])[C@@H:3]([NH:7][C:8]1[CH:9]=[N:10][CH:11]=[CH:12][CH:13]=1)[C:4]([OH:6])=O.[Cl:15][C:16]1[CH:21]=[CH:20][C:19]([C@@:22]2([OH:30])[CH2:27][CH2:26][NH:25][CH2:24][C:23]2([CH3:29])[CH3:28])=[CH:18][CH:17]=1.C(Cl)CCl.C1C=CC2N(O)N=NC=2C=1.CCN(C(C)C)C(C)C>CN(C=O)C>[Cl:15][C:16]1[CH:21]=[CH:20][C:19]([C@@:22]2([OH:30])[CH2:27][CH2:26][N:25]([C:4](=[O:6])[C@H:3]([NH:7][C:8]3[CH:9]=[N:10][CH:11]=[CH:12][CH:13]=3)[CH:2]([CH3:1])[CH3:14])[CH2:24][C:23]2([CH3:28])[CH3:29])=[CH:18][CH:17]=1

参加物

7

反応物 5

HCID 111,2-DichloroethaneHCID 757711-HydroxybenzotriazoleHCID 81531DiisopropylethylamineHCID 18437142(S)-4-(4-chlorophenyl)-3,3-dimethylpiperidin-4-olHCID 57889332HCID 57889332、化合物

生成物 1

HCID 57889973HCID 57889973、化合物収率 6.5%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

(R)-3-Methyl-2-(pyridine-3-ylamino)butanoic acid (162 mg, 0.83 mmol), (S)-4-(4-chlorophenyl)-3,3-dimethylpiperidin-4-ol (200 mg, 0.83 mmol), EDC (320 mg, 1.67 mmol), HOBT (113 mg, 0.83 mmol), DIPEA (431 mg, 3.34 mmol), and DMF (4 mL) was stirred overnight at rt. Example 607 was isolated as a greenish solid using preparative reverse phase HPLC (22.5 mg, 6.5% yield). M+H=416.18.

後処理

  1. customExample 607 was isolated as a greenish solid

出典と根拠

ORDレコード
ord-de3f74e18e144e55997f203afcd8f56a
出典データセット
uspto-grants-2011_07
特許番号
US07985861B2

反応ノート

読み込み中…