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

HRID 57643노트

반응식

HRID 57643 반응식
[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

참가 물질

4

반응물 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

생성물 1

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

시약·촉매·용매 1

HCID 8857Ethyl Acetate용매2회

실험 절차

(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)+

후처리

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

출처 및 근거

ORD 기록
ord-35ba6ce6decb45c7869092108a8f920f
출처 데이터셋
uspto-grants-2016_09
특허 번호
US09434726B2

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