3,5-Bis(difluoromethyl)-1H-pyrazole-1-acetic acid → 2-{3-[2-(1-{[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2-oxazol-5-yl}-benzaldehyde

HRID 409946

反応式

HRID 409946 の反応式
[Cl-].[CH:2]([C:4]1[CH:9]=[CH:8][CH:7]=[CH:6][C:5]=1[CH:10]1[O:14][N:13]=[C:12]([C:15]2[N:16]=[C:17]([CH:20]3[CH2:25][CH2:24][NH2+:23][CH2:22][CH2:21]3)[S:18][CH:19]=2)[CH2:11]1)=[O:3].[F:26][CH:27]([F:40])[C:28]1[CH:32]=[C:31]([CH:33]([F:35])[F:34])[N:30]([CH2:36][C:37](O)=[O:38])[N:29]=1>>[F:40][CH:27]([F:26])[C:28]1[CH:32]=[C:31]([CH:33]([F:35])[F:34])[N:30]([CH2:36][C:37]([N:23]2[CH2:24][CH2:25][CH:20]([C:17]3[S:18][CH:19]=[C:15]([C:12]4[CH2:11][CH:10]([C:5]5[CH:6]=[CH:7][CH:8]=[CH:9][C:4]=5[CH:2]=[O:3])[O:14][N:13]=4)[N:16]=3)[CH2:21][CH2:22]2)=[O:38])[N:29]=1

参加物

3

反応物 2

HCID 12298443,5-Bis(difluoromethyl)-1H-pyrazole-1-acetic acidHCID 178519461HCID 178519461、化合物

生成物 1

HCID 866575662-{3-[2-(1-{[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]-4,5-dihydro-1,2-oxazol-5-yl}-benzaldehyde

実験手順

4-{4-[5-(2-Formylphenyl)-4,5-dihydro-1,2-oxazol-3-yl]-1,3-thiazol-2-yl}piperidinium chloride (433 mg) and [3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]acetic acid (285 mg) were reacted analogously to I-40 (step 3). This gave 2-{3-[2-(1-{[3,5-bis(difluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-O-1,3-thiazol-4-yl]-4,5-dihydro-1,2-oxazol-5-yl}benzaldehyde (330 mg).

出典と根拠

ORDレコード
ord-6d927205360743d0a103329fc7a23125
出典データセット
uspto-grants-2014_06
特許番号
US08759527B2

関連ノート

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