Pyrazole → (r)-4-Bromo-5-(2-chlorobenzoylamino)-1-methyl-pyrazole-3-carboxylic acid (1,5-dimethyl-2-oxo-2,3,4,5-tetrahydro-1h-benzo[b][1,4]diazepin-3-yl)amide

反応式

N1C=C[CH:3]=N1.[CH3:6][N:7]([C@@H:26]([C:28]1C=CC=C[CH:29]=1)C)[C:8](C1C(Br)=C(NC(=O)C2C=CC=CC=2Cl)NN=1)=[O:9].[Cl:34][C:35]1[CH:43]=[CH:42][CH:41]=[CH:40][C:36]=1[C:37](Cl)=[O:38].[N:44]1([CH2:49][CH2:50][NH:51][C:52]([C:54]2[C:58]([Br:59])=[C:57]([NH:60]C(=O)C3C=CC=CC=3Cl)[NH:56][N:55]=2)=[O:53])[CH2:48][CH2:47][CH2:46][CH2:45]1>>[CH3:6][N:7]1[C:8](=[O:9])[C@H:50]([NH:51][C:52]([C:54]2[C:58]([Br:59])=[C:57]([NH:60][C:37](=[O:38])[C:36]3[CH:40]=[CH:41][CH:42]=[CH:43][C:35]=3[Cl:34])[N:56]([CH3:3])[N:55]=2)=[O:53])[CH2:49][N:44]([CH3:45])[C:48]2[CH:47]=[CH:46][CH:29]=[CH:28][C:26]1=2

参加物

反応物 4

HCID 1048Pyrazole

HCID 691102-Chlorobenzoyl chloride

HCID 178461679HCID 178461679、化合物

HCID 178522629HCID 178522629、化合物

生成物 1

HCID 59773391(r)-4-Bromo-5-(2-chlorobenzoylamino)-1-methyl-pyrazole-3-carboxylic acid (1,5-dimethyl-2-oxo-2,3,4,5-tetrahydro-1h-benzo[b][1,4]diazepin-3-yl)amide

実験手順

The pyrazole acid, prepared by coupling methyl ester 85 (Gen. Proc. 26) with 2-chlorobenzoyl chloride (21) followed by hydrolysis and bromination as shown in Gen. Proc. 8. was coupled to compound 92 (Procedure 27) using the method of Procedure 3.

後処理

customfollowed by hydrolysis and bromination

出典と根拠

ORDレコード: ord-f916f3bd86ef43c9848028e3ab5e0dd9
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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