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Methylboronic Acid → [4-(3,5-Dimethylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-ylmethyl)-2-methylphenyl]methanone

HRID 2411851
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HRID 2411851 반응식
Br[C:2]1[CH:7]=[C:6]([CH2:8][N:9]2[CH2:13][CH2:12][CH2:11][S:10]2(=[O:15])=[O:14])[CH:5]=[CH:4][C:3]=1[C:16]([N:18]1[CH2:23][CH2:22][N:21]([C:24]2[C:29]([CH3:30])=[CH:28][C:27]([CH3:31])=[CH:26][N:25]=2)[CH2:20][CH2:19]1)=[O:17].[CH3:32]B(O)O>>[CH3:30][C:29]1[C:24]([N:21]2[CH2:22][CH2:23][N:18]([C:16]([C:3]3[CH:4]=[CH:5][C:6]([CH2:8][N:9]4[CH2:13][CH2:12][CH2:11][S:10]4(=[O:15])=[O:14])=[CH:7][C:2]=3[CH3:32])=[O:17])[CH2:19][CH2:20]2)=[N:25][CH:26]=[C:27]([CH3:31])[CH:28]=1
참가 물질실험 절차출처 및 근거반응 노트

참가 물질

3

반응물 2

HCID 139377Methylboronic AcidHCID 71252686[2-Bromo-4-(1,1-dioxo-1lambda6-isothiazolidin-2-ylmethyl)phenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone

생성물 1

HCID 71252566[4-(3,5-Dimethylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-ylmethyl)-2-methylphenyl]methanone수율 86%

실험 절차

Using [2-bromo-4-(1,1-dioxo-1λ6-isothiazolidin-2-ylmethyl)phenyl][4-(3,5-dimethylpyridin-2-yl)piperazin-1-yl]methanone (120 mg) described in Example 461 and methylboronic acid (42 mg) and by the reaction and treatment in the same manner as in Example 115, the title compound (90 mg) was obtained.

출처 및 근거

ORD 기록
ord-f2ba55900b2a4b0f98f686633ce503de
출처 데이터셋
uspto-grants-2014_08
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US08816079B2

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