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Iodoethane → (R)-7-(4-(1-ethylpiperidin-4-yl)phenyl)-N-((4-(methylsulfonyl)morpholin-2-yl)methyl)pyrido[4,3-b]pyrazin-5-amine

HRID 57646
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HRID 57646 반응식
[CH3:1][S:2]([N:5]1[CH2:10][CH2:9][O:8][C@H:7]([CH2:11][NH:12][C:13]2[C:22]3[C:17](=[N:18][CH:19]=[CH:20][N:21]=3)[CH:16]=[C:15]([C:23]3[CH:28]=[CH:27][C:26]([CH:29]4[CH2:34][CH2:33][NH:32][CH2:31][CH2:30]4)=[CH:25][CH:24]=3)[N:14]=2)[CH2:6]1)(=[O:4])=[O:3].C([O-])([O-])=O.[K+].[K+].I[CH2:42][CH3:43]>CN(C=O)C.CC(=O)OCC>[CH2:42]([N:32]1[CH2:33][CH2:34][CH:29]([C:26]2[CH:25]=[CH:24][C:23]([C:15]3[N:14]=[C:13]([NH:12][CH2:11][C@H:7]4[O:8][CH2:9][CH2:10][N:5]([S:2]([CH3:1])(=[O:3])=[O:4])[CH2:6]4)[C:22]4[C:17](=[N:18][CH:19]=[CH:20][N:21]=4)[CH:16]=3)=[CH:28][CH:27]=2)[CH2:30][CH2:31]1)[CH3:43]
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참가 물질

6

반응물 3

HCID 6340IodoethaneHCID 11430Potassium CarbonateHCID 86717407(R)-N-((4-(methylsulfonyl)morpholin-2-yl)methyl)-7-(4-(piperidin-4-yl)phenyl)pyrido[4,3-b]pyrazin-5-amine

생성물 1

HCID 86717406(R)-7-(4-(1-ethylpiperidin-4-yl)phenyl)-N-((4-(methylsulfonyl)morpholin-2-yl)methyl)pyrido[4,3-b]pyrazin-5-amine

시약·촉매·용매 2

HCID 6228
Dimethylformamide
용매
HCID 8857Ethyl Acetate용매

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온도
100 °C

실험 절차

To a solution of (R)—N-((4-(methylsulfonyl)morpholin-2-yl)methyl)-7-(4-(piperidin-4-yl)phenyl)pyrido[4,3-b]pyrazin-5-amine in (39.5 mg, 0.082 mmol) in DMF (5 mL) was added K2CO3 (22.6 mg, 0.164 mmol) and iodoethane (25.5 mg, 0.164 mmol) at room temperature. The reaction was stirred at 100° C. for 18 hours. After that, the reaction was dissolved in 50 mL of EA, washed with H2O (25 mL) and brine (25 mL), dried over Na2SO4 and concentrated, purified on TLC (CH2Cl2:MeOH=20:1) to give yellow solid. MS (m/z): 511 (M+H)+

후처리

  1. washwashed with H2O (25 mL) and brine (25 mL)
  2. dry with materialdried over Na2SO4
  3. concentrationconcentrated
  4. custompurified on TLC (CH2Cl2:MeOH=20:1)
  5. customto give yellow solid

출처 및 근거

ORD 기록
ord-94db86058942461489343301fbea363f
출처 데이터셋
uspto-grants-2016_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09434726B2

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