合成路线:Coupling of methacryloyl chloride (I) with substituted aniline (II) in dimethylacetamide yields amide (III),which is then converted into the epoxy derivative (IV) by oxidation with m-chloroperbenzoic acid (mCPBA) and 4-methyl-2,6-di-tert-butylphenol (A) in refluxing 1,1,1-trichloroethane.Condensation of (IV) with thiol (V) by means of NaH in THF provides fluorophenylthio derivative (VI),which is finally oxidized with mCPBA in CH2Cl2 to furnish the desired compound trichloroethane.
参考文献标题:Nonsteroidal antiandrogens.Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides
文献作者:Tucker,H.; Crook,J.W.; Chesterson,G.J.
参考来源:J Med Chem 1988,31(5),954
合成路线:The reaction of 4-amino-2-(trifluoromethyl)benzonitrile (I) with 2-oxopropionic acid (II) by means of SOCl2 gives the corresponding amide (III),which is finally condensed with the methyl sulfone (IV) by means of BuLi in THF.
参考文献标题:A two-step synthesis of the anti-cancer drug (R,S)-bicalutamide
文献作者:Ekwuribe,N.N.; James,K.D.
参考来源:Synthesis (Stuttgart) 2002,(7),850
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