1,2-Dichloroethane → 3(S)-(2,3-Dihydro-benzofuran-6-yl)-3-(3-(1,2,3,4,6,7,8,9-octahydro-benzo[b][1,8]naphthyridin-8-yl)-propionylamino)-propionic acid ethyl ester

HRID 1004268ノート

反応式

HRID 1004268 の反応式
[NH:1]1[C:10]2[N:9]=[C:8]3[CH2:11][CH:12]([CH2:15][CH2:16][C:17]([OH:19])=O)[CH2:13][CH2:14][C:7]3=[CH:6][C:5]=2[CH2:4][CH2:3][CH2:2]1.[CH2:20]([O:22][C:23](=[O:36])[CH2:24][C@H:25]([NH2:35])[C:26]1[CH:34]=[CH:33][C:29]2[CH2:30][CH2:31][O:32][C:28]=2[CH:27]=1)[CH3:21].C(Cl)CCl.C1C=CC2N(O)N=NC=2C=1.CN1CCOCC1>CN(C=O)C>[CH2:20]([O:22][C:23](=[O:36])[CH2:24][C@@H:25]([C:26]1[CH:34]=[CH:33][C:29]2[CH2:30][CH2:31][O:32][C:28]=2[CH:27]=1)[NH:35][C:17](=[O:19])[CH2:16][CH2:15][CH:12]1[CH2:11][C:8]2=[N:9][C:10]3[NH:1][CH2:2][CH2:3][CH2:4][C:5]=3[CH:6]=[C:7]2[CH2:14][CH2:13]1)[CH3:21]

参加物

7

反応物 5

HCID 111,2-DichloroethaneHCID 79724-MethylmorpholineHCID 757711-HydroxybenzotriazoleHCID 108236463(S)-Amino-3-(2,3-dihydro-benzofuran-6-yl)-propionic acid ethyl esterHCID 226781623-(1,2,3,4,6,7,8,9-Octahydro-benzo[b][1,8]naphthyridin-8-yl)-propionic acid

生成物 1

HCID 698949923(S)-(2,3-Dihydro-benzofuran-6-yl)-3-(3-(1,2,3,4,6,7,8,9-octahydro-benzo[b][1,8]naphthyridin-8-yl)-propionylamino)-propionic acid ethyl ester

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

A solution of 14-4 (0.110 g, 0.39 mmol), β-aminoester 6-6 (0.106 g 0.39 mmol), EDC (0.075 g, 0.39 mmol), HOBT (0.053 g, 0.39 mmol) and N-methylmorpholine (0.164 mL, 1.17 mmol) in degassed DMF (5 mL) was stirred at room temperature for 12 h. The solution was concentrated. The residue was purified by flash chromatography to give 14-5.

後処理

  1. concentrationThe solution was concentrated
  2. customThe residue was purified by flash chromatography
  3. customto give 14-5

出典と根拠

ORDレコード
ord-77014a70af4743929e35b1ef5ae6940c
出典データセット
uspto-grants-2000_04
特許番号
US06048861

反応ノート

読み込み中…