2-{2-Ethyl-4-[5-(5-isobutyl-4-methyl-pyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-6-methyl-phenoxy}-ethylamine → Ethanesulfonic acid (2-{2-ethyl-4-[5-(5-isobutyl-4-methyl-pyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-6-methyl-phenoxy}-ethyl)-amide

HRID 2037376ノート

反応式

HRID 2037376 の反応式
[CH2:1]([C:3]1[CH:12]=[C:11]([C:13]2[N:17]=[C:16]([C:18]3[CH:23]=[C:22]([CH3:24])[C:21]([CH2:25][CH:26]([CH3:28])[CH3:27])=[CH:20][N:19]=3)[O:15][N:14]=2)[CH:10]=[C:9]([CH3:29])[C:4]=1[O:5][CH2:6][CH2:7][NH2:8])[CH3:2].[K+].[CH2:31]([S:33]([NH-])(=[O:35])=[O:34])[CH3:32]>CN(C=O)C>[CH2:1]([C:3]1[CH:12]=[C:11]([C:13]2[N:17]=[C:16]([C:18]3[CH:23]=[C:22]([CH3:24])[C:21]([CH2:25][CH:26]([CH3:28])[CH3:27])=[CH:20][N:19]=3)[O:15][N:14]=2)[CH:10]=[C:9]([CH3:29])[C:4]=1[O:5][CH2:6][CH2:7][NH:8][S:33]([CH2:31][CH3:32])(=[O:35])=[O:34])[CH3:2]

参加物

4

反応物 2

HCID 442181592-{2-Ethyl-4-[5-(5-isobutyl-4-methyl-pyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-6-methyl-phenoxy}-ethylamineHCID 59645266Ethanesulfonamide potassium salt

生成物 1

HCID 91366116Ethanesulfonic acid (2-{2-ethyl-4-[5-(5-isobutyl-4-methyl-pyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-6-methyl-phenoxy}-ethyl)-amide収率 19.4%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

A solution of the methanesulfonic acid ester intermediate of Example 48 (25 mg, 53 μmol) and ethanesulfonamide potassium salt (16 mg, 106 μmol) in DMF (2 mL) is stirred at 60° C. for 18 h. The mixture is concentrated and separated by prep. HPLC to give the title compound (5 mg) as a colourless oil; LC-MS: tR=1.14 min, [M+H]+=487.14.

後処理

  1. concentrationThe mixture is concentrated
  2. customseparated by prep

出典と根拠

ORDレコード
ord-32b1c678ba0d4570a1070c70bc09d209
出典データセット
uspto-grants-2013_11
特許番号
US08575200B2

反応ノート

読み込み中…