Morpholine → [6-Bromo-5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]-morpholin-4-yl-methanone

HRID 19886노트

반응식

HRID 19886 반응식
FC1(F)CCN(C(C2NC3C(C=2)=CC(OC2CCN(C(C)C)CC2)=CC=3)=O)CC1.Cl.BrC1C=C2C(C=C(C(O)=O)N2)=CC=1OC1CCN(C(C)C)CC1.[Br:54][C:55]1[CH:63]=[C:62]2[C:58]([CH:59]=[C:60]([C:71]([N:73]3[CH2:78][CH2:77][O:76][CH2:75][CH2:74]3)=[O:72])[N:61]2C2C=CN=C(Cl)C=2)=[CH:57][C:56]=1[O:79][CH:80]1[CH2:85][CH2:84][N:83]([CH:86]([CH3:88])[CH3:87])[CH2:82][CH2:81]1.N1CCOCC1>>[Br:54][C:55]1[CH:63]=[C:62]2[C:58]([CH:59]=[C:60]([C:71]([N:73]3[CH2:78][CH2:77][O:76][CH2:75][CH2:74]3)=[O:72])[NH:61]2)=[CH:57][C:56]=1[O:79][CH:80]1[CH2:81][CH2:82][N:83]([CH:86]([CH3:88])[CH3:87])[CH2:84][CH2:85]1

참가 물질

5

반응물 4

HCID 8083MorpholineHCID 11603838(4,4-Difluoropiperidin-1-yl)[5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]methanoneHCID 16739659[6-Bromo-1-(2-chloro-pyridin-4-yl)-5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]-morpholin-4-yl-methanoneHCID 670179306-bromo-5-(1-isopropyl-piperidin-4-yloxy)-1H-indole-2-carboxylic acid hydrochloride

생성물 1

HCID 67017918[6-Bromo-5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]-morpholin-4-yl-methanone

실험 절차

In analogy to the procedure described for the synthesis of intermediate 1, step 4, the title compound was synthesized from 6-bromo-5-(1-isopropyl-piperidin-4-yloxy)-1H-indole-2-carboxylic acid hydrochloride salt with 1 eq. lithium chloride (example 41, step 5) and morpholine. The title compound was obtained in 75% yield as light yellow solid. MS (m/e): 450.1 (MH+, 100%).

출처 및 근거

ORD 기록
ord-15bf8b8fe03e41a0b9141f752a51aa86
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07745479B2

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