3,4-Dichlorobenzeneboronic acid → (1-(3,4-dichlorophenyl)-5-(1-isopropylpiperidin-4-yloxy)-1H-indol-2-yl)(4,4-difluoropiperidin-1-yl)methanone

HRID 19861

反応式

HRID 19861 の反応式
[F:1][C:2]1([F:29])[CH2:7][CH2:6][N:5]([C:8]([C:10]2[NH:11][C:12]3[C:17]([CH:18]=2)=[CH:16][C:15]([O:19][CH:20]2[CH2:25][CH2:24][N:23]([CH:26]([CH3:28])[CH3:27])[CH2:22][CH2:21]2)=[CH:14][CH:13]=3)=[O:9])[CH2:4][CH2:3]1.[Cl:30][C:31]1[CH:32]=[C:33](B(O)O)[CH:34]=[CH:35][C:36]=1[Cl:37]>>[Cl:30][C:31]1[CH:32]=[C:33]([N:11]2[C:12]3[C:17](=[CH:16][C:15]([O:19][CH:20]4[CH2:25][CH2:24][N:23]([CH:26]([CH3:27])[CH3:28])[CH2:22][CH2:21]4)=[CH:14][CH:13]=3)[CH:18]=[C:10]2[C:8]([N:5]2[CH2:6][CH2:7][C:2]([F:1])([F:29])[CH2:3][CH2:4]2)=[O:9])[CH:34]=[CH:35][C:36]=1[Cl:37]

参加物

3

反応物 2

HCID 27343303,4-Dichlorobenzeneboronic acidHCID 11603838(4,4-Difluoropiperidin-1-yl)[5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]methanone2 回

生成物 1

HCID 16739525(1-(3,4-dichlorophenyl)-5-(1-isopropylpiperidin-4-yloxy)-1H-indol-2-yl)(4,4-difluoropiperidin-1-yl)methanone

実験手順

In analogy to the procedure described for the synthesis of example 6, the title compound was synthesized from (4,4-difluoro-piperidin-1-yl)-[5-(1-isopropyl-piperidin-4-yloxy)-1H-indol-2-yl]-methanone (intermediate 1) and 3,4-dichlorophenylboronic acid. The title compound was obtained in 81% yield as yellow foam. MS (m/e): 550.2 (MH+, 100%).

後処理

  1. customIn analogy to the procedure described for the synthesis of example 6

出典と根拠

ORDレコード
ord-d4bb8722977941e6945f970d1a5873ce
出典データセット
uspto-grants-2010_06
特許番号
US07745479B2

関連ノート

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