DB-480-药物合成数据库

【药物名称】DB-480

化学结构式(Chemical Structure):

参考文献No.	40514
标题:	2,4-Bis (4-amidino)phenyl furans as anti-Pneumocystis carinii agents
作者:	Boykin, D.W.; Francesconi, I.; Tidwell, R.R.; Wilson, D.W. (Georgia State University; University of North Carolina)
来源:	EP 0941991; GB 2334716; US 6008247

合成路线图解说明: Aldol condensation of 4-cyanobenzaldehyde (II) with 4-cyano-acetophenone (I) in methanolic NaOH furnished chalcone (III). Subsequent addition of bromine to (III) gave dibromide (IV). This was treated with NaOMe to produce the intermediate enol ether (V), which was then condensed with the ylide generated from trimethylsulfonium iodide and NaH to afford the 2,4-diarylfuran (VI). Acid-catalyzed addition of EtOH to (VI) provided the corresponding bis(imidate) (VII). Further reaction of (VII) with isopropylamine yielded the target amidine, which was isolated as the dihydrochloride salt.

参考文献No.	541844
标题:	2,4-Diphenyl furan diamidines as novel anti-pneumocystis carinii pneumonia agents
作者:	Francesconi, I.; Wilson, W.D.; Tanious, F.A.; Hall, J.E.; Bender, B.C.; Tidwell, R.R.; McCurdy, D.; Boykin, D.W.
来源:	J Med Chem 1999,42(12),2260

合成路线图解说明: Aldol condensation of 4-cyanobenzaldehyde (II) with 4-cyano-acetophenone (I) in methanolic NaOH furnished chalcone (III). Subsequent addition of bromine to (III) gave dibromide (IV). This was treated with NaOMe to produce the intermediate enol ether (V), which was then condensed with the ylide generated from trimethylsulfonium iodide and NaH to afford the 2,4-diarylfuran (VI). Acid-catalyzed addition of EtOH to (VI) provided the corresponding bis(imidate) (VII). Further reaction of (VII) with isopropylamine yielded the target amidine, which was isolated as the dihydrochloride salt.