Cesium carbonate → [1-(4-Chloro-phenyl)-cyclobutyl]-{3-[4-(2-fluoro-phenyl)-piperazin-1-ylmethyl]-piperidin-1-yl}-methanone

HRID 50650

反応式

HRID 50650 の反応式
[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2([C:12]([N:14]3[CH2:19][CH2:18][CH2:17][CH:16]([CH2:20]OS(C)(=O)=O)[CH2:15]3)=[O:13])[CH2:11][CH2:10][CH2:9]2)=[CH:4][CH:3]=1.[F:26][C:27]1[CH:32]=[CH:31][CH:30]=[CH:29][C:28]=1[N:33]1[CH2:38][CH2:37][NH:36][CH2:35][CH2:34]1.C(=O)([O-])[O-].[Cs+].[Cs+]>>[Cl:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2([C:12]([N:14]3[CH2:19][CH2:18][CH2:17][CH:16]([CH2:20][N:36]4[CH2:35][CH2:34][N:33]([C:28]5[CH:29]=[CH:30][CH:31]=[CH:32][C:27]=5[F:26])[CH2:38][CH2:37]4)[CH2:15]3)=[O:13])[CH2:11][CH2:10][CH2:9]2)=[CH:4][CH:3]=1

参加物

4

反応物 3

HCID 10796Cesium carbonateHCID 705291-(2-Fluorophenyl)piperazineHCID 12992442Methanesulfonic acid 1-[1-(4-chloro-phenyl)-cyclobutanecarbonyl]-piperidin-3-ylmethyl ester

生成物 1

HCID 12992446[1-(4-Chloro-phenyl)-cyclobutyl]-{3-[4-(2-fluoro-phenyl)-piperazin-1-ylmethyl]-piperidin-1-yl}-methanone収率 46%

実験手順

Compound 8 was prepared using the method described in Example 3, starting with compound 2 (1.0 g, 2.60 mmol), 1-(2-fluorophenyl)piperazine (0.51 g, 2.86 mmol), and cesium carbonate (1.27 g, 3.90 mmol) to give 8 (0.56 g, 46%); C27H33ClFN3O, LRMS (m/z)=471 (MH+).

後処理

  1. customCompound 8 was prepared

出典と根拠

ORDレコード
ord-1aaa49faf76d44e2b39252fbc683a6bf
出典データセット
uspto-grants-2004_03
特許番号
US06713479B2

関連ノート

読み込み中…