1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride → 5-Chloro-1H-indole-7-carboxylic acid (4-tert-butyl-benzyl)-[2-(4-fluoro-phenyl)-ethyl]-amide

HRID 855456

반응식

HRID 855456 반응식
[C:1]([C:5]1[CH:21]=[CH:20][C:8]([CH2:9][NH:10][CH2:11][CH2:12][C:13]2[CH:18]=[CH:17][C:16]([F:19])=[CH:15][CH:14]=2)=[CH:7][CH:6]=1)([CH3:4])([CH3:3])[CH3:2].[Cl:22][C:23]1[CH:24]=[C:25]2[C:29](=[C:30]([C:32](O)=[O:33])[CH:31]=1)[NH:28][CH:27]=[CH:26]2.CCN=C=NCCCN(C)C.Cl>C(Cl)Cl>[C:1]([C:5]1[CH:21]=[CH:20][C:8]([CH2:9][N:10]([CH2:11][CH2:12][C:13]2[CH:18]=[CH:17][C:16]([F:19])=[CH:15][CH:14]=2)[C:32]([C:30]2[CH:31]=[C:23]([Cl:22])[CH:24]=[C:25]3[C:29]=2[NH:28][CH:27]=[CH:26]3)=[O:33])=[CH:7][CH:6]=1)([CH3:4])([CH3:2])[CH3:3]

참가 물질

5

반응물 3

HCID 27239391,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 29280418(4-Tert-butyl-benzyl)-[2-(4-fluoro-phenyl)-ethyl]-amineHCID 668685635-chloro-1H-indole-7-carboxylic acid

생성물 1

HCID 866031365-Chloro-1H-indole-7-carboxylic acid (4-tert-butyl-benzyl)-[2-(4-fluoro-phenyl)-ethyl]-amide수율 64%

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

140 mg (0.5 mmol) of (4-tert-butyl-benzyl)-[2-(4-fluoro-phenyl)-ethyl]-amine, 97 mg (0.5 mmol) of 5-chloro-1H-indole-7-carboxylic acid and 115 mg (0.6 mmol) of EDC.HCl were stirred over night at rt in 10 ml DCM. The product was purified by column chromatography (20 silica gel; DCM) to yield 140 mg (64%) product as a colorless oil. MS (EI) 462.2 (27), 463.2 (14), 464.2 (12) (M)+.

후처리

  1. customThe product was purified by column chromatography (20 silica gel; DCM)

출처 및 근거

ORD 기록
ord-519331fdce9a4a71bc9b24a174014064
출처 데이터셋
uspto-grants-2007_08
특허 번호
US07259183B2

연결된 노트

불러오는 중…