N4-[4-(tert-Butyl)-1,3-thiazol-2-yl]-2-aminoisonicotinamide → N8-[4-(tert-butyl)-1,3-thiazol-2-yl]-2,4-dioxo-3,4-dihydro-2H-pyrido[1,2-a]pyrimidine-8-carboxamide

HRID 1828442노트

반응식

HRID 1828442 반응식
[C:1]([C:5]1[N:6]=[C:7]([NH:10][C:11](=[O:19])[C:12]2[CH:17]=[CH:16][N:15]=[C:14]([NH2:18])[CH:13]=2)[S:8][CH:9]=1)([CH3:4])([CH3:3])[CH3:2].[C:20](OC1C=CC(Cl)=C(Cl)C=1Cl)(=[O:25])[CH2:21][C:22]([O-])=[O:23]>C1(C)C(C)=CC=CC=1>[C:1]([C:5]1[N:6]=[C:7]([NH:10][C:11]([C:12]2[CH:17]=[CH:16][N:15]3[C:20](=[O:25])[CH2:21][C:22](=[O:23])[N:18]=[C:14]3[CH:13]=2)=[O:19])[S:8][CH:9]=1)([CH3:4])([CH3:2])[CH3:3]

참가 물질

4

반응물 2

HCID 22063525N4-[4-(tert-Butyl)-1,3-thiazol-2-yl]-2-aminoisonicotinamideHCID 22063717Trichlorophenyl malonate

생성물 1

HCID 22063754N8-[4-(tert-butyl)-1,3-thiazol-2-yl]-2,4-dioxo-3,4-dihydro-2H-pyrido[1,2-a]pyrimidine-8-carboxamide수율 84%

시약·촉매·용매 1

HCID 7237O-Xylene용매

반응 조건

온도
130 °C

실험 절차

N4-[4-(tert-Butyl)-1,3-thiazol-2-yl]-2-aminoisonicotinamide (200 mg, 0.724 mmol) was added with xylene (20 ml) and trichlorophenyl malonate (370 mg, 0.796 mmol) and refluxed by heating at 130° C. The reaction solution was stirred for 1 hour, then returned to room temperature and concentrated under reduced pressure. The resulting orange crystals was taken by filtration, washed with chloroform, dried under reduced pressure to obtain 209 mg (84%) of the title compound as orange crystals without purification.

후처리

  1. temperaturerefluxed
  2. customreturned to room temperature
  3. concentrationconcentrated under reduced pressure
  4. filtrationThe resulting orange crystals was taken by filtration
  5. washwashed with chloroform
  6. customdried under reduced pressure

출처 및 근거

ORD 기록
ord-fcd8f059b5fe4effa3a35423e0f94982
출처 데이터셋
uspto-grants-2006_06
특허 번호
US07056917B2

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