17-Hydroxy-13-methyl-2,14-dioxo-3,13,15-triaza-tricyclo[13.3.0.0*4,6*]octadec-7-ene-4-carboxylic acid ethyl ester → 17-[2-(4-Fluoro-phenyl)-7-methoxy-8-methyl-quinazolin-4-yloxy]-13-methyl-2,14-dioxo-3,13,15-triaza-tricyclo[13.3.0.0*4,6*]octadec-7-ene-4-carboxylic acid
반응식
[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[N:17]=[C:16]([OH:18])[C:15]3[C:10](=[C:11]([CH3:21])[C:12]([O:19][CH3:20])=[CH:13][CH:14]=3)[N:9]=2)=[CH:4][CH:3]=1.C([O:24][C:25]([C:27]12[CH2:44][CH:43]1[CH:42]=[CH:41][CH2:40][CH2:39][CH2:38][CH2:37][N:36]([CH3:45])[C:35](=[O:46])[N:34]1[CH:30]([CH2:31][CH:32](O)[CH2:33]1)[C:29](=[O:48])[NH:28]2)=[O:26])C>>[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2[N:17]=[C:16]([O:18][CH:32]3[CH2:31][CH:30]4[N:34]([C:35](=[O:46])[N:36]([CH3:45])[CH2:37][CH2:38][CH2:39][CH2:40][CH:41]=[CH:42][CH:43]5[C:27]([C:25]([OH:26])=[O:24])([NH:28][C:29]4=[O:48])[CH2:44]5)[CH2:33]3)[C:15]3[C:10](=[C:11]([CH3:21])[C:12]([O:19][CH3:20])=[CH:13][CH:14]=3)[N:9]=2)=[CH:6][CH:7]=1참가 물질
3
반응물 2
생성물 1
실험 절차
Quinazolinol derivative (92) (141 mg, 0.5 mmol) was coupled to compound 51 (170 mg, 0.45 mmol) as described in example 52, which gave the crude ethyl ester of the title compound. The crude ester was purified by flash chromatography on silica gel eluted with 5→15% MeOH in diethyl ether, the afforded residue was dissolved in dichloromethane and filtered to remove traces of silica, which gave the ethyl ester of the title compound (135 mg, 46%). The ethyl ester was then hydrolyzed as described in example 52, which gave the title compound (125 mg, 100%)
출처 및 근거
- ORD 기록
- ord-6053d68f4f274d6488f10a2958701a08
- 출처 데이터셋
- uspto-grants-2010_02
- 특허 번호
- US07659245B2
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