2-(Trifluoromethyl)benzylamine → Pyrido[4,3-d]pyrimidine-4,7-diamine,n4-[[2-(trifluoromethyl)phenyl]methyl]-

HRID 50814

반응식

HRID 50814 반응식
[NH2:1][C:2]1[N:11]=[CH:10][C:9]2[C:8](SC)=[N:7][CH:6]=[N:5][C:4]=2[CH:3]=1.[F:14][C:15]([F:25])([F:24])[C:16]1[CH:23]=[CH:22][CH:21]=[CH:20][C:17]=1[CH2:18][NH2:19]>>[NH2:1][C:2]1[N:11]=[CH:10][C:9]2[C:8]([NH:19][CH2:18][C:17]3[CH:20]=[CH:21][CH:22]=[CH:23][C:16]=3[C:15]([F:14])([F:24])[F:25])=[N:7][CH:6]=[N:5][C:4]=2[CH:3]=1

참가 물질

3

반응물 2

HCID 764472-(Trifluoromethyl)benzylamineHCID 104425627-Amino-4-methylthiopyrido[4,3-d]pyrimidine

생성물 1

HCID 5328084Pyrido[4,3-d]pyrimidine-4,7-diamine,n4-[[2-(trifluoromethyl)phenyl]methyl]-수율 59%

반응 조건

온도
150 °C

실험 절차

A mixture of 7-amino-4-methylthiopyrido[4,3-d]pyrimidine (225 mg, 1.17 mmol) and 2-(trifluoromethyl)benzylamine (0.90 mL, 6.42 mmol) is stirred under N2 at 150° C. for 1 h. The resulting product is chromatographed on silica gel (5% EtOH/EtOAc) to give 7-amino-4-(2-trifluoromethylbenzyl) aminopyrido[4,3-d]pyrimidine (0.22 g, 59%) as a white solid. 1H NMR (DMSO) δ 9.16 (1H, s), 8.88 (1H, t, J=5.7 Hz), 8.23 (1H, s), 7.75 (1H, d, J=7.7 Hz), 7.62 (1H, t, J=7.5 Hz), 7.50 (1H, d, J=7.4 Hz), 7.47 (1H, t, J=7.6 Hz), 6.51 (2H, brs), 6.39 (1H, s), 4.92 (2H, d, J=5.5 Hz).

후처리

  1. customThe resulting product is chromatographed on silica gel (5% EtOH/EtOAc)

출처 및 근거

ORD 기록
ord-e97f24bc52184d6abfb510c91e17a213
출처 데이터셋
uspto-grants-2004_03
특허 번호
US06713484B2

연결된 노트

불러오는 중…