4-Toluenesulfonyl chloride → 2-(4-fluorophenyl)-4-tosyloxy-5-[4-(methylsulfonyl)phenyl]-3(2H)-pyridazinone

HRID 1241805ノート

反応式

HRID 1241805 の反応式
FC1C=CC(N2C(=O)C(OC)=C(Br)C=N2)=CC=1.FC1C=CC(N2C(=O)C(OC)=C(C3C=CC(SC)=CC=3)C=N2)=CC=1.[F:42][C:43]1[CH:48]=[CH:47][C:46]([N:49]2[C:54](=[O:55])[C:53]([OH:56])=[C:52]([C:57]3[CH:62]=[CH:61][C:60]([S:63]([CH3:66])(=[O:65])=[O:64])=[CH:59][CH:58]=3)[CH:51]=[N:50]2)=[CH:45][CH:44]=1.[OH-].[Na+].[C:69]1([CH3:79])[CH:74]=[CH:73][C:72]([S:75](Cl)(=[O:77])=[O:76])=[CH:71][CH:70]=1>>[F:42][C:43]1[CH:48]=[CH:47][C:46]([N:49]2[C:54](=[O:55])[C:53]([O:56][S:75]([C:72]3[CH:73]=[CH:74][C:69]([CH3:79])=[CH:70][CH:71]=3)(=[O:77])=[O:76])=[C:52]([C:57]3[CH:62]=[CH:61][C:60]([S:63]([CH3:66])(=[O:64])=[O:65])=[CH:59][CH:58]=3)[CH:51]=[N:50]2)=[CH:45][CH:44]=1

参加物

6

反応物 5

HCID 73974-Toluenesulfonyl chlorideHCID 14798Sodium HydroxideHCID 14874955-bromo-2-(4-fluorophenyl)-4-methoxy-3(2H)-pyridazinoneHCID 219341922-(4-Fluorophenyl)-4-methoxy-5-[4-(methylthio)phenyl]-3(2H)-pyridazinoneHCID 178504687HCID 178504687、化合物

生成物 1

HCID 219338542-(4-fluorophenyl)-4-tosyloxy-5-[4-(methylsulfonyl)phenyl]-3(2H)-pyridazinone

実験手順

2-(4-Fluorophenyl)-4-methoxy-5-bromo-3(2H)-pyridazinone (Example 194B) was converted into 2-(4-fluorophenyl)-4-methoxy-5-[4-(methylthio)phenyl]-3(2H)-pyridazinone according to the method of Example 194C followed by the oxidation method in Example 10. The methoxy compound was converted to the 2-(4-fluorophenyl)-4-hydroxy-5-[4-(methylsulfonyl)phenyl]-3(2H)-pyridazinone, by treatment with NaOH according to the procedure of Example 332. The hydroxy compound was treated with p-toluenesulfonyl chloride according to the procedure of Example 333, to furnish 2-(4-fluorophenyl)-5-[4-(methylsulfonyl)phenyl]-4-tosyloxy-3(2H)-pyridazinone.

出典と根拠

ORDレコード
ord-eb5a8f14ded24112b749aa38851a81ab
出典データセット
uspto-grants-2006_10
特許番号
US07115591B2

反応ノート

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