Pyrazole → Ethylenediamine

反応式

[NH:1]1[CH:5]=CC=N1.C[N:7]([C@@H:26](C1C=CC=CC=1)[CH3:27])[C:8]([C:10]1[C:14]([Br:15])=[C:13]([NH:16][C:17](=[O:25])[C:18]2[CH:23]=[CH:22][CH:21]=[CH:20][C:19]=2[Cl:24])[NH:12][N:11]=1)=[O:9].Cl[C:35]1C=[CH:42][CH:41]=[CH:40][C:36]=1C(Cl)=O.N[CH2:45]CC1C=CC(C#N)=CC=1>>[CH2:10]([NH2:11])[CH2:8][NH2:7].[CH3:5][N:1]1[CH2:42][CH2:41][CH:40]([CH2:27][CH2:26][NH:7][C:8]([C:10]2[C:14]([Br:15])=[C:13]([NH:16][C:17](=[O:25])[C:18]3[CH:23]=[CH:22][CH:21]=[CH:20][C:19]=3[Cl:24])[N:12]([CH3:45])[N:11]=2)=[O:9])[CH2:36][CH2:35]1

参加物

反応物 4

HCID 1048Pyrazole

HCID 691102-Chlorobenzoyl chloride

HCID 219125254-(2-Aminoethyl)benzonitrile

HCID 178461679HCID 178461679、化合物

生成物 2

HCID 3301Ethylenediamine

HCID 597735024-Bromo-5-(2-chloro-benzoylamino)-1-methyl-pyrazole-3-carboxylic acid [2-(n-methyl-piperidin-4-yl)-ethyl]amide

実験手順

The pyrazole acid, prepared by coupling methyl ester 85 (Procedure 26) with 2-chlorobenzoyl chloride (21) followed by hydrolysis and bromination as shown in Procedure 8, was coupled to amine 169 (Procedure 34) using the method of Procedure 10. Formation of the amidine using the method of Procedure 33 using ethylene diamine afforded the title compound.

後処理

customfollowed by hydrolysis and bromination

出典と根拠

ORDレコード: ord-b9336c3ccaec44958ecafe2ee00a4297
出典データセット: uspto-grants-2008_10
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07432379B2

反応ノート

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