2-Fluorobenzoic acid → N-[2-[4-[[3-butyl-5-oxo-1-[5-(propanoylamino)-2-(trifluoromethyl)phenyl]-1,2,4-triazol-4-yl]methyl]-3-fluorophenyl]phenyl]sulfonyl-2-fluorobenzamide

HRID 36306

反応式

[CH2:1]([C:5]1[N:6]([CH2:26][C:27]2[CH:32]=[CH:31][C:30]([C:33]3[CH:38]=[CH:37][CH:36]=[CH:35][C:34]=3[S:39](=[O:42])(=[O:41])[NH2:40])=[CH:29][C:28]=2[F:43])[C:7](=[O:25])[N:8]([C:10]2[CH:15]=[C:14]([NH:16][C:17](=[O:20])[CH2:18][CH3:19])[CH:13]=[CH:12][C:11]=2[C:21]([F:24])([F:23])[F:22])[N:9]=1)[CH2:2][CH2:3][CH3:4].[F:44][C:45]1[CH:53]=[CH:52][CH:51]=[CH:50][C:46]=1[C:47](O)=[O:48].C1N=CN(C(N2C=NC=C2)=O)C=1.C1CCN2C(=NCCC2)CC1>CN(C1C=CN=CC=1)C>[CH2:1]([C:5]1[N:6]([CH2:26][C:27]2[CH:32]=[CH:31][C:30]([C:33]3[CH:38]=[CH:37][CH:36]=[CH:35][C:34]=3[S:39](=[O:41])(=[O:42])[NH:40][C:47](=[O:48])[C:46]3[CH:50]=[CH:51][CH:52]=[CH:53][C:45]=3[F:44])=[CH:29][C:28]=2[F:43])[C:7](=[O:25])[N:8]([C:10]2[CH:15]=[C:14]([NH:16][C:17](=[O:20])[CH2:18][CH3:19])[CH:13]=[CH:12][C:11]=2[C:21]([F:24])([F:22])[F:23])[N:9]=1)[CH2:2][CH2:3][CH3:4]

参加物

実験手順

Reaction of 5-n-butyl-2,4-dihydro-4-[(3-fluoro-2'-sulfamoyl-biphenyl-4-yl)methyl]-2-[5-(propionylamino)-2-(trifluoromethyl)phenyl]-3H-1,2,4-triazol-3-one (from Step C) with 2-fluorobenzoic acid (3 equivalents), CDI (3 equiv), DBU (3 equiv), and DMAP (3 equiv) according to the method of Example 51 (as modified in Example 81) gave a a 93% yield of the title compound as a white, stiff foam, mp 119°-122° C.; homogeneous by TLC in 9:1 CH2Cl2 --MeOH; mass spectrum (FAB) m/e 742 (M+1)+.

出典と根拠

ORDレコード: ord-0857376cb8d44a71bf1bd924fb40b46d
出典データセット: uspto-grants-1995_05
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US05411980

反応式

参加物

反応物 4

生成物 1

試薬・触媒・溶媒 1

実験手順

出典と根拠

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