N1-(3-fluoro-4-(thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-phenylmalonamide → (R)-N1-(4-(2-(3-(dimethylamino)pyrrolidine-1-carbonyl)thieno[3,2-b]pyridin-7-yloxy)-3-fluorophenyl)-N3-phenylmalonamide

HRID 2193660

반응식

HRID 2193660 반응식
[F:1][C:2]1[CH:3]=[C:4]([NH:18][C:19](=[O:30])[CH2:20][C:21]([NH:23][C:24]2[CH:29]=[CH:28][CH:27]=[CH:26][CH:25]=2)=[O:22])[CH:5]=[CH:6][C:7]=1[O:8][C:9]1[CH:14]=[CH:13][N:12]=[C:11]2[CH:15]=[CH:16][S:17][C:10]=12.FC1C=C(N)C=CC=1OC1C=CN=C2C=C(C3N(C)C=CN=3)SC=12.NC1C=CC(OC2C=CN=C3C=C([C:70]([N:72]4[CH2:76][CH2:75][C@@H:74]([N:77]([CH3:79])[CH3:78])[CH2:73]4)=[O:71])SC=23)=C(F)C=1>>[CH3:78][N:77]([CH3:79])[C@@H:74]1[CH2:75][CH2:76][N:72]([C:70]([C:16]2[S:17][C:10]3[C:11](=[N:12][CH:13]=[CH:14][C:9]=3[O:8][C:7]3[CH:6]=[CH:5][C:4]([NH:18][C:19](=[O:30])[CH2:20][C:21]([NH:23][C:24]4[CH:25]=[CH:26][CH:27]=[CH:28][CH:29]=4)=[O:22])=[CH:3][C:2]=3[F:1])[CH:15]=2)=[O:71])[CH2:73]1

참가 물질

4

반응물 3

HCID 45488043N1-(3-fluoro-4-(thieno[3,2-b]pyridin-7-yloxy)phenyl)-N3-phenylmalonamideHCID 58790294(R)-(7-(4-Amino-2-fluorophenoxy)thieno[3,2-b]pyridin-2-yl)(3-(dimethylamino) pyrrolidin-1-yl)methanoneHCID 594244803-Fluoro-4-(2-(1-methyl-1H-imidazol-2-yl)thieno[3,2-b]pyridin-7-yloxy)benzenamine

생성물 1

HCID 45488073(R)-N1-(4-(2-(3-(dimethylamino)pyrrolidine-1-carbonyl)thieno[3,2-b]pyridin-7-yloxy)-3-fluorophenyl)-N3-phenylmalonamide수율 38%

실험 절차

Following the procedure described above for the compound 5a (step 5, example 1) but replacing the amine 9 with the compound 26, title compound 5g was obtained in 38% yield. MS (m/z): 562.0 (M+H).

출처 및 근거

ORD 기록
ord-a96a3ca557084838bc358ddf4215f0e9
출처 데이터셋
uspto-grants-2012_12
특허 번호
US08329726B2

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