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4-Methylpyridine-3-Boronic Acid → [7-(4-Methyl-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-(4-morpholin-4-yl-phenyl)-amine

HRID 1262192
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HRID 1262192 반응식
Br[C:2]1[N:10]2[C:5]([CH:6]=[N:7][C:8]([NH:11][C:12]3[CH:17]=[CH:16][C:15]([N:18]4[CH2:23][CH2:22][O:21][CH2:20][CH2:19]4)=[CH:14][CH:13]=3)=[N:9]2)=[CH:4][CH:3]=1.[CH3:24][C:25]1[CH:30]=[CH:29][N:28]=[CH:27][C:26]=1B(O)O>>[CH3:24][C:25]1[CH:30]=[CH:29][N:28]=[CH:27][C:26]=1[C:2]1[N:10]2[C:5]([CH:6]=[N:7][C:8]([NH:11][C:12]3[CH:13]=[CH:14][C:15]([N:18]4[CH2:23][CH2:22][O:21][CH2:20][CH2:19]4)=[CH:16][CH:17]=3)=[N:9]2)=[CH:4][CH:3]=1
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반응물 2

HCID 27627114-Methylpyridine-3-Boronic AcidHCID 54578326(7-Bromo-pyrrolo[2,1-f][1,2,4]triazin-2-yl)-(4-morpholin-4-yl-phenyl)-amine

생성물 1

HCID 66712482[7-(4-Methyl-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-(4-morpholin-4-yl-phenyl)-amine

실험 절차

[7-(4-Methyl-pyridin-3-yl)-pyrrolo[2,1-f][1,2,4]triazin-2-yl]-(4-morpholin-4-yl-phenyl)-amine was prepared from (7-bromo-pyrrolo[2,1-f][1,2,4]triazin-2-yl)-(4-morpholin-4-yl-phenyl)-amine and 4-methylpyridine-3-boronic acid in an analogous manner to Example 1031b. Product isolated as a yellow solid (55 mg, 48%). m.p.=191-193° C.; LCMS (m/e) 387 (M+H); 1H-NMR (CDCl3, 400 MHz) δ 8.76-8.69 (m, 2H), 8.59-8.52 (m, 1H), 7.37 (d, 2H, J=7.40 Hz), 7.31-7.26 (m, 1H), 6.88-6.84 (m, 1H), 6.84-6.75 (m, 3H), 6.67 (s, 1H), 3.89-3.81 (m, 4H), 3.12-3.04 (m, 4H), 2.31 (s, 3H).

출처 및 근거

ORD 기록
ord-66e7dcc8c6aa455f894240937afe3cc3
출처 데이터셋
uspto-grants-2013_06
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08471005B2

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