Isoxazolidine hydrochloride → 6-Cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carboxylic acid [5-(isoxazolidine-2-carbonyl)-1-methyl-1H-pyrazol-4-yl]-amide

HRID 467790

反応式

HRID 467790 の反応式
[CH:1]1([C:4]2[N:9]=[C:8]([C:10]([NH:12][C:13]3[CH:17]=[N:16][N:15]([CH3:18])[C:14]=3[C:19]([OH:21])=O)=[O:11])[C:7]([NH:22][C:23]3[CH:24]=[N:25][CH:26]=[N:27][CH:28]=3)=[N:6][CH:5]=2)[CH2:3][CH2:2]1.Cl.[O:30]1[CH2:34][CH2:33][CH2:32][NH:31]1>>[O:30]1[CH2:34][CH2:33][CH2:32][N:31]1[C:19]([C:14]1[N:15]([CH3:18])[N:16]=[CH:17][C:13]=1[NH:12][C:10]([C:8]1[C:7]([NH:22][C:23]2[CH:28]=[N:27][CH:26]=[N:25][CH:24]=2)=[N:6][CH:5]=[C:4]([CH:1]2[CH2:3][CH2:2]2)[N:9]=1)=[O:11])=[O:21]

参加物

3

反応物 2

HCID 12304500Isoxazolidine hydrochlorideHCID 700980734-{[6-Cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carbonyl]-amino}-2-methyl-2H-pyrazole-3-carboxylic acid

生成物 1

HCID 547609416-Cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carboxylic acid [5-(isoxazolidine-2-carbonyl)-1-methyl-1H-pyrazol-4-yl]-amide

実験手順

The product was obtained starting from 4-{[6-cyclopropyl-3-(pyrimidin-5-ylamino)-pyrazine-2-carbonyl]-amino}-2-methyl-2H-pyrazole-3-carboxylic acid (50 mg, 131 μmol; example 236, step 3) and isoxazolidine hydrochloride (17 mg, 145 μmol) according to the method described in example 64, step 6 after purification by preparative HPLC using an acetonitrile/water gradient as yellow solid (9 mg, 16%).

後処理

  1. customThe product was obtained
  2. customafter purification by preparative HPLC

出典と根拠

ORDレコード
ord-135d1f9fd190444c9420077e946ddaae
出典データセット
uspto-grants-2014_01
特許番号
US08623866B2

関連ノート

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