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8532059 
Journal Article 
Synthesis of bazedoxifene acetate 
Chen, S; Liu, XK; Yu, X; Yuan, ZD 
2013 
22 
13 
1571-1573+1590 
Chinese 
Objective: To synthesize osteoporosis therapeutic agent bazedoxifene acetate. Methods: Bazedoxifene acetate was synthesized via ten steps. The side chain was got by condensation, reduction and chlorination starting from p-hydroxybenzaldehyde and 2-(hexamethyleneimino)ethyl chloride hydrochloride. The parent nucleus was obtained by condensation, bromination, condensation and cyclization taking p-hydroxypropiophenone as raw material. The obtained side chain and parent nucleus were condensed and processed by hydrogenolysis and acidification to get the objective compound. Results: The chemical structure of the target compound was confirmed by MS and 1H-NMR. The total yield was 18.1%. Conclusion: This synthetic process is mild and simple, which is feasible for industrialization. 
Bazedoxifene acetate; Osteoporosis; Postmenopausal women; Selective estrogen receptor modulator; Synthesis