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

HRID 1788075
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HRID 1788075 반응식
[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]([F:42])([F:41])[O:28][C:29]1[CH:34]=[CH:33][CH:32]=[CH:31][C:30]=1[N:35]1[CH2:40][CH2:39][NH:38][CH2:37][CH2:36]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:38]4[CH2:39][CH2:40][N:35]([C:30]5[CH:31]=[CH:32][CH:33]=[CH:34][C:29]=5[O:28][C:27]([F:26])([F:41])[F:42])[CH2:36][CH2:37]4)[CH2:15]3)=[O:13])[CH2:11][CH2:10][CH2:9]2)=[CH:4][CH:3]=1
참가 물질실험 절차후처리출처 및 근거반응 노트

참가 물질

4

반응물 3

HCID 10796Cesium carbonateHCID 107529251-(2-Trifluoromethoxyphenyl)piperazineHCID 12992442Methanesulfonic acid 1-[1-(4-chloro-phenyl)-cyclobutanecarbonyl]-piperidin-3-ylmethyl ester

생성물 1

HCID 12992447[1-(4-Chloro-phenyl)-cyclobutyl]-{3-[4-(2-trifluoromethoxy-phenyl)-piperazin-1-ylmethyl]-piperidin-1-yl}-methanone수율 32.3%

실험 절차

Compound 9 was prepared using the method described in Example 3, starting with compound 2 (1.0 g, 2.60 mmol), 1-(2-trifluoromethoxyphenyl)piperazine (0.70 g, 2.86 mmol), and cesium carbonate (1.27 g, 3.90 mmol) to give 9 (0.45 g, 32%); C28H33ClF3N3O2, LRMS (m/z)=537 (MH+).

후처리

  1. customCompound 9 was prepared

출처 및 근거

ORD 기록
ord-1eff77d0a8f94fd79d80d99e54259ac7
출처 데이터셋
uspto-grants-2009_03
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07511141B2

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