Acetone → Bazedoxifene
반응식
[CH3:1][C:2]1[C:3]2[CH:4]=[C:5]([OH:35])[CH:6]=[CH:7][C:8]=2[N:9]([CH2:18][C:19]2[CH:20]=[CH:21][C:22]([O:25][CH2:26][CH2:27][N:28]3[CH2:34][CH2:33][CH2:32][CH2:31][CH2:30][CH2:29]3)=[CH:23][CH:24]=2)[C:10]=1[C:11]1[CH:12]=[CH:13][C:14]([OH:17])=[CH:15][CH:16]=1.C(OC1C=C2C(=CC=1)N(CC1C=CC(OCCBr)=CC=1)C(C1C=CC(OCC3C=CC=CC=3)=CC=1)=C2C)C1C=CC=CC=1.N1CCCCCC1.CC(C)=O>C(O)(=O)C>[CH3:1][C:2]1[C:3]2[CH:4]=[C:5]([OH:35])[CH:6]=[CH:7][C:8]=2[N:9]([CH2:18][C:19]2[CH:24]=[CH:23][C:22]([O:25][CH2:26][CH2:27][N:28]3[CH2:29][CH2:30][CH2:31][CH2:32][CH2:33][CH2:34]3)=[CH:21][CH:20]=2)[C:10]=1[C:11]1[CH:12]=[CH:13][C:14]([OH:17])=[CH:15][CH:16]=1참가 물질
5
실험 절차
European Patent Application No. 0802183 describes a synthesis of bazedoxifene 5-Benzyloxy-2(4-benzyloxyphenyl)-1-[4-(2-bromoethoxy)benzyl]-3-methyl-indole is reacted with azepan, under suitable reaction conditions, followed by deprotection to yield bazedoxifene, which on subsequent treatment with acetone and acetic acid gives bazedoxifene acetate.