1-Methylpiperazine → [3,5-Difluoro-4-(4-methoxy-benzylamino)-phenyl]-(4-methyl-piperazin-1-yl)-methanone

反応式

[F:1][C:2]1[CH:3]=[C:4]([CH:8]=[C:9]([F:21])[C:10]=1[NH:11][CH2:12][C:13]1[CH:18]=[CH:17][C:16]([O:19][CH3:20])=[CH:15][CH:14]=1)[C:5]([OH:7])=O.[CH3:22][N:23]1[CH2:28][CH2:27][NH:26][CH2:25][CH2:24]1>>[F:21][C:9]1[CH:8]=[C:4]([C:5]([N:26]2[CH2:27][CH2:28][N:23]([CH3:22])[CH2:24][CH2:25]2)=[O:7])[CH:3]=[C:2]([F:1])[C:10]=1[NH:11][CH2:12][C:13]1[CH:18]=[CH:17][C:16]([O:19][CH3:20])=[CH:15][CH:14]=1

参加物

反応物 2

HCID 531671-Methylpiperazine

HCID 592447773,5-Difluoro-4-(4-methoxy-benzylamino)-benzoic acid

生成物 1

HCID 59244847[3,5-Difluoro-4-(4-methoxy-benzylamino)-phenyl]-(4-methyl-piperazin-1-yl)-methanone

実験手順

Using 3,5-difluoro-4-(4-methoxy-benzylamino)-benzoic acid (95.4 mg) obtained in Step B in Example 1-D-24 and 1-methyl-piperazine (43.3 μl) instead of 1-ethyl-piperazine, in the same manner as Step C in Example 1-D-24, the desired compound was obtained as a crude product (82 mg, 67%).

出典と根拠

ORDレコード: ord-cdab4e8553384ab8b7bb6ed9dc182ca4
出典データセット: uspto-grants-2011_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08022205B2

反応ノート

読み込み中…