Ethanesulfonamide potassium salt → Ethanesulfonic acid ((2s)-3-{2-ethyl-4-[5-(5-isobutyl-4-methyl-pyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-6-methyl-phenoxy}-2-hydroxy-propyl)-amide

HRID 2037379

反応式

HRID 2037379 の反応式
[CH2:1]([C:3]1[CH:15]=[C:14]([C:16]2[N:20]=[C:19]([C:21]3[CH:26]=[C:25]([CH3:27])[C:24]([CH2:28][CH:29]([CH3:31])[CH3:30])=[CH:23][N:22]=3)[O:18][N:17]=2)[CH:13]=[C:12]([CH3:32])[C:4]=1[O:5][CH2:6][C@@H:7]([OH:11])[CH2:8][NH:9]C)[CH3:2].[K+].[CH2:34]([S:36]([NH-])(=[O:38])=[O:37])[CH3:35]>CN(C=O)C>[CH2:1]([C:3]1[CH:15]=[C:14]([C:16]2[N:20]=[C:19]([C:21]3[CH:26]=[C:25]([CH3:27])[C:24]([CH2:28][CH:29]([CH3:30])[CH3:31])=[CH:23][N:22]=3)[O:18][N:17]=2)[CH:13]=[C:12]([CH3:32])[C:4]=1[O:5][CH2:6][C@@H:7]([OH:11])[CH2:8][NH:9][S:36]([CH2:34][CH3:35])(=[O:38])=[O:37])[CH3:2]

参加物

4

反応物 2

HCID 59645266Ethanesulfonamide potassium saltHCID 68629918(s)-1-{2-Ethyl-4-[5-(5-isobutyl-4-methyl-pyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-6-methyl-phenoxy}-3-methylamino-propan-2-ol

生成物 1

HCID 44218630Ethanesulfonic acid ((2s)-3-{2-ethyl-4-[5-(5-isobutyl-4-methyl-pyridin-2-yl)-[1,2,4]oxadiazol-3-yl]-6-methyl-phenoxy}-2-hydroxy-propyl)-amide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

A solution of the epoxide intermediate of Example 57 (step a, 25 mg, 61 μmol) and ethanesulfonamide potassium salt (27 mg, 184 μmol) in DMF (2 mL) is stirred at 60° C. for 18 h. The solvent is removed in vacuo and the crude product is purified by prep. HPLC to give the title compound (8 mg) as a colourless oil; LC-MS: tR=1.07 min, [M+H]+=517.12.

後処理

  1. customThe solvent is removed in vacuo
  2. customthe crude product is purified by prep

出典と根拠

ORDレコード
ord-802634dd8cf04804a5038a1714dbcfb3
出典データセット
uspto-grants-2013_11
特許番号
US08575200B2

関連ノート

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