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 379248ノート

反応式

HRID 379248 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-500aae137bf941058b50396cd10df6a8
出典データセット
uspto-grants-2001_10
特許番号
US06297249B1

反応ノート

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