1-Hydroxybenzotriazole → HCID 11486710、化合物

HRID 2103762

反応式

HRID 2103762 の反応式
[CH3:1][C:2]([CH3:21])([CH3:20])[C:3]([C:5]1[O:6][C:7]2[CH:17]=[CH:16][C:15]([O:18][CH3:19])=[CH:14][C:8]=2[C:9]=1[CH2:10][C:11](O)=[O:12])=[O:4].C1C=CC2N(O)N=NC=2C=1.[CH2:32]1[C@@H:41]2[C@@H:36]([CH2:37][CH2:38][CH2:39][CH2:40]2)[CH2:35][CH2:34][NH:33]1.CCN(C(C)C)C(C)C>CN(C=O)C.C(Cl)CCl>[CH3:19][O:18][C:15]1[CH:16]=[CH:17][C:7]2[O:6][C:5]([C:3](=[O:4])[C:2]([CH3:21])([CH3:1])[CH3:20])=[C:9]([CH2:10][C:11]([N:33]3[CH2:34][CH2:35][C@H:36]4[C@H:41]([CH2:40][CH2:39][CH2:38][CH2:37]4)[CH2:32]3)=[O:12])[C:8]=2[CH:14]=1

参加物

7

反応物 4

HCID 757711-HydroxybenzotriazoleHCID 81531DiisopropylethylamineHCID 11062467cis-DecahydroisoquinolineHCID 57804476[2-(2,2-Dimethylpropanoyl)-5-methoxy-1-benzofuran-3-yl]acetic acid

生成物 1

HCID 11486710HCID 11486710、化合物

試薬・触媒・溶媒 2

HCID 111,2-Dichloroethane溶媒HCID 6228Dimethylformamide溶媒

反応条件

温度
40 °C

実験手順

Dissolve a mixture of 17 mg [2-(2,2-dimethylpropanoyl)-5-methoxy-1-benzofuran-3-yl]acetic acid from the Step B Example 1 and 18.5 mg HOBt in 1 mL dry DMF. Add 12.3 mg cis-decahydroisoquinoline followed by 23.0 mg EDC and 35 μL DIEA. This solution was heated at 40° C. for 2 hours. It was purified directly on RP-HPLC using 65-100% MeCN gradient. The fractions containing pure product were pooled and lyophilized to give the title compound. LC-MS: 4.41 min. (m/Z=412.3, 328.2, 434.2).

後処理

  1. dissolutionDissolve
  2. customIt was purified directly on RP-HPLC using 65-100% MeCN gradient
  3. additionThe fractions containing pure product

出典と根拠

ORDレコード
ord-31aaaa5308304e29bc5ce33f5fe7b0dd
出典データセット
uspto-grants-2009_08
特許番号
US07576122B2

関連ノート

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