2-Methoxy-4-morpholinoaniline → 2-Methoxy-3-[4-(2-methoxy-4-morpholin-4-yl-phenylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one

HRID 1687853

반응식

Cl[C:2]1[C:7]([C:8]([F:11])([F:10])[F:9])=[CH:6][N:5]=[C:4]([NH:12][C:13]2[C:25]([O:26][CH3:27])=[CH:24][C:16]3[CH2:17][CH2:18][O:19][C:20](=[O:23])[N:21]([CH3:22])[C:15]=3[CH:14]=2)[N:3]=1.[CH3:28][O:29][C:30]1[CH:35]=[C:34]([N:36]2[CH2:41][CH2:40][O:39][CH2:38][CH2:37]2)[CH:33]=[CH:32][C:31]=1[NH2:42]>>[CH3:27][O:26][C:25]1[C:13]([NH:12][C:4]2[N:3]=[C:2]([NH:42][C:31]3[CH:32]=[CH:33][C:34]([N:36]4[CH2:37][CH2:38][O:39][CH2:40][CH2:41]4)=[CH:35][C:30]=3[O:29][CH3:28])[C:7]([C:8]([F:11])([F:10])[F:9])=[CH:6][N:5]=2)=[CH:14][C:15]2[N:21]([CH3:22])[C:20](=[O:23])[O:19][CH2:18][CH2:17][C:16]=2[CH:24]=1

참가 물질

반응물 2

HCID 4149602-Methoxy-4-morpholinoaniline

HCID 866340553-(4-Chloro-5-trifluoromethyl-pyrimidin-2-ylamino)-2-methoxy-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one

생성물 1

HCID 668306902-Methoxy-3-[4-(2-methoxy-4-morpholin-4-yl-phenylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one수율 43%

실험 절차

In an analogous manner to Example 1513, the product was prepared from 3-(4-Chloro-5-trifluoromethyl-pyrimidin-2-ylamino)-2-methoxy-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one and 2-Methoxy-4-morpholin-4-yl-phenylamine. Product was isolated as a white solid (55 mg, 43%). mp: 221-223° C., MS (ESI+): 575 (M+H), 1H-NMR (CDCl3, 400 MHz) δ 8.38 (s, 1H), 8.30 (s, 1H), 7.83 (s, 1H), 7.68 (s, 1H), 7.60 (br d, 1H), 7.03 (s, 1H), 6.63 (s, 1H), 6.32 (br d, 1H), 4.36 (t, J=6 Hz, 2H), 3.82 (s, 3H), 3.78 (s, 3H), 3.75 (m, 4H), 3.11 (m, 4H), 3.01 (s, 3H), 2.93 (t, J=6 Hz, 2H).

출처 및 근거

ORD 기록: ord-878d89094c734d08afbff2407dd487fe
출처 데이터셋: uspto-grants-2012_04
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US08148391B2

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