【药物名称】Dofequidar fumarate, MS-209
化学结构式(Chemical Structure):
参考文献No.424081
标题:Structure-activity relationship of newly synthesiz
作者:Suzuki, T.; Fukazawa, N.; San-nohe, K.; Sato, W.; Yano, O.; Tsuruo, T.
来源:J Med Chem 1997,40(13),2047
合成路线图解说明:

N-(2,2-Diphenylacetyl)piperazine (IV) was prepared by acylation of N-formylpiperazine (II) with 2,2-diphenylacetyl chloride (I), followed by acid-promoted formyl deprotection of the resulting amide (III). Condensation of 5-hydroxyquinoline (VI) with epichlorohydrin (V) in the presence of potassium tert-butoxide in DMF at 90 C provided 5-(2,3-epoxypropoxy)quinoline (VII), which was subsequently coupled with acylpiperazine (IV) in boiling isopropanol to yield (VIII). This was finally treated with fumaric acid (IX) in MeOH to furnish the title sesquifumarate salt.

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