【药物名称】Tefluxitol, Lu-10-022
化学结构式(Chemical Structure):
参考文献No.900302
标题:
作者:Buus, J.M.L.; Lassen, N.; Bigler, A.J.
来源:AT 332395; AT 345826; BE 845057; CA 1010870; DE 2359359; FR 2209573; FR 2320740; GB 1453828; GB 1498394; JP 7494691; JP 7739682; NL 7316035; NL 7608822; US 4042695; US 4044024; ZA 7308990; ZA 7604544
合成路线图解说明:

The condensation of 2-chloro-5-trifluoromethylbenzonitrile (I) with 3-fluorothiophenol (II) by means of sodium ethoxide in refluxing ethanol gives 2-(3-fluorophenylthio)-5-trifluoromethylbenzoic acid (III), which is cyclized by means of H2SO4 at 65 C yielding 6-fluoro-2-trifluoromethylthioxanthone (IV). The Grignard reaction of (IV) with 3-dimethylaminopropylmagnesium chloride (V) in refluxing THF affords 6-fluoro-2-trifluoromethyl-9-(3-dimethylaminopropyl)thioxanthene (VII). The condensation of (VII) with N-(2-hydroxyethyl)piperazine (VIII) in isopropanol at 140 C yields 6-fluoro-2-trifluoro-9-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propylidene]thioxanthene (IX), which is finally reduced with aqueous HI and red P in refluxing acetic acid.

参考文献No.950049
标题:Teflutixol
作者:Blancafort, P.; Serradell, M.N.; Casta馿r, J.; Owen, R.T.
来源:Drugs Fut 1982,7(6),410
合成路线图解说明:

The condensation of 2-chloro-5-trifluoromethylbenzonitrile (I) with 3-fluorothiophenol (II) by means of sodium ethoxide in refluxing ethanol gives 2-(3-fluorophenylthio)-5-trifluoromethylbenzoic acid (III), which is cyclized by means of H2SO4 at 65 C yielding 6-fluoro-2-trifluoromethylthioxanthone (IV). The Grignard reaction of (IV) with 3-dimethylaminopropylmagnesium chloride (V) in refluxing THF affords 6-fluoro-2-trifluoromethyl-9-(3-dimethylaminopropyl)thioxanthene (VII). The condensation of (VII) with N-(2-hydroxyethyl)piperazine (VIII) in isopropanol at 140 C yields 6-fluoro-2-trifluoro-9-[3-[4-(2-hydroxyethyl)piperazin-1-yl]propylidene]thioxanthene (IX), which is finally reduced with aqueous HI and red P in refluxing acetic acid.

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