1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-amine → (R)-N,N-dimethyl-2-(4-(1-(thiazol-2-ylmethyl)-1H-indazol-5-ylamino)quinazolin-5-yloxy)propanamide

HRID 1162230노트

반응식

HRID 1162230 반응식
[CH3:1][N:2]([CH3:19])[C:3](=[O:18])[C@H:4]([O:6][C:7]1[CH:16]=[CH:15][CH:14]=[C:13]2[C:8]=1[C:9](=O)[NH:10][CH:11]=[N:12]2)[CH3:5].[S:20]1[CH:24]=[CH:23][N:22]=[C:21]1[CH2:25][N:26]1[C:34]2[C:29](=[CH:30][C:31]([NH2:35])=[CH:32][CH:33]=2)[CH:28]=[N:27]1>>[CH3:1][N:2]([CH3:19])[C:3](=[O:18])[C@H:4]([O:6][C:7]1[CH:16]=[CH:15][CH:14]=[C:13]2[C:8]=1[C:9]([NH:35][C:31]1[CH:30]=[C:29]3[C:34](=[CH:33][CH:32]=1)[N:26]([CH2:25][C:21]1[S:20][CH:24]=[CH:23][N:22]=1)[N:27]=[CH:28]3)=[N:10][CH:11]=[N:12]2)[CH3:5]

참가 물질

3

반응물 2

HCID 686192881-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-amineHCID 136346624(2R)-N,N-dimethyl-2-[(4-oxo-3,4-dihydroquinazolin-5-yl)oxy]propanamide

생성물 1

HCID 16117349(R)-N,N-dimethyl-2-(4-(1-(thiazol-2-ylmethyl)-1H-indazol-5-ylamino)quinazolin-5-yloxy)propanamide수율 77.1%

실험 절차

Using the same procedure as in Example 18, (2R)—N,N-dimethyl-2-[(4-oxo-3,4-dihydroquinazolin-5-yl)oxy]propanamide (150 mg, 0.57 mmol) and 1-(1,3-thiazol-2-ylmethyl)-1H-indazol-5-amine (138 mg, 0.6 mmol) were reacted to give the title compound as a white solid (208 mg, 77%); NMR Spectrum (CDCl3) 1.73 (d, 3H), 3.06 (s, 3H), 3.14 (s, 3H), 5.43 (q, 1H), 5.92 (s, 2H), 6.82 (d, 1H), 7.26 (m, 1H), 7.50 (d, 2H), 7.61 (t, 1H), 7.75 (d, 1H), 7.87 (dd, 1H), 8.11 (s, 1H), 8.45 (s, 1H), 8.62 (s, 1H); Mass spectrum 474.

후처리

  1. customwere reacted

출처 및 근거

ORD 기록
ord-67c836bd132b4dcf894a49bea5b1eb64
출처 데이터셋
uspto-grants-2010_10
특허 번호
US07820683B2

반응 노트

불러오는 중…