Pyrazole → Ethylenediamine

HRID 2114312노트

반응식

HRID 2114312 반응식
[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

참가 물질

6

반응물 4

HCID 1048PyrazoleHCID 691102-Chlorobenzoyl chlorideHCID 219125254-(2-Aminoethyl)benzonitrileHCID 178461679HCID 178461679, 화합물

생성물 2

HCID 3301EthylenediamineHCID 597735024-Bromo-5-(2-chloro-benzoylamino)-1-methyl-pyrazole-3-carboxylic acid [2-(n-methyl-piperidin-4-yl)-ethyl]amide

실험 절차

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.

후처리

  1. customfollowed by hydrolysis and bromination

출처 및 근거

ORD 기록
ord-b9336c3ccaec44958ecafe2ee00a4297
출처 데이터셋
uspto-grants-2008_10
특허 번호
US07432379B2

반응 노트

불러오는 중…