Hydrochloric Acid → (S)-1-(4-(5-(morpholin-2-ylmethylamino)pyrido[4,3-b]pyrazin-7-yl)phenyl)piperidin-4-ol

HRID 57643ノート

反応式

HRID 57643 の反応式
[OH:1][CH:2]1[CH2:7][CH2:6][N:5]([C:8]2[CH:13]=[CH:12][C:11]([C:14]3[N:23]=[C:22]([NH:24][CH2:25][C@H:26]4[O:31][CH2:30][CH2:29][N:28](C(OC(C)(C)C)=O)[CH2:27]4)[C:21]4[C:16](=[N:17][CH:18]=[CH:19][N:20]=4)[CH:15]=3)=[CH:10][CH:9]=2)[CH2:4][CH2:3]1.Cl>CC(=O)OCC>[NH:28]1[CH2:29][CH2:30][O:31][C@H:26]([CH2:25][NH:24][C:22]2[C:21]3[C:16](=[N:17][CH:18]=[CH:19][N:20]=3)[CH:15]=[C:14]([C:11]3[CH:10]=[CH:9][C:8]([N:5]4[CH2:6][CH2:7][CH:2]([OH:1])[CH2:3][CH2:4]4)=[CH:13][CH:12]=3)[N:23]=2)[CH2:27]1

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 86717400(R)-tert-butyl 2-((7-(4-(4-hydroxypiperidin-1-yl)phenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate

生成物 1

HCID 86717401(S)-1-(4-(5-(morpholin-2-ylmethylamino)pyrido[4,3-b]pyrazin-7-yl)phenyl)piperidin-4-ol収率 45.3%

試薬・触媒・溶媒 1

HCID 8857Ethyl Acetate溶媒2 回

実験手順

(R)-tert-butyl 2-((7-(4-(4-hydroxypiperidin-1-yl)phenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate (112 mg, 0.21 mmol) was dissolved in 20 mL EA, then 15 mL 5M HCl in EA was added in. The mixture was stirred at room temperature overnight, concentrated, treated with ammonia, purified by preparative TLC to give 40 mg reddish solid. MS: (m/z): 421 (M+H)+

後処理

  1. concentrationconcentrated
  2. additiontreated with ammonia
  3. custompurified by preparative TLC

出典と根拠

ORDレコード
ord-35ba6ce6decb45c7869092108a8f920f
出典データセット
uspto-grants-2016_09
特許番号
US09434726B2

反応ノート

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