【药物名称】
化学结构式(Chemical Structure):
参考文献No.553518
标题:Synthesis and evaluation of analogs of efavirenz (Sustiva(TM)) as HIV-1 reverse transcriptase inhibitors
作者:Patel, M.; Ko, S.S.; McHugh, R.J. Jr.; Markwalder, J.A.; Srivastava, A.S.; Cordova, B.C.; Klabe, R.M.; Erickson-Vittanen, S.; Trainor, G.L.; Seitz, S.P.
来源:Bioorg Med Chem Lett 1999,9(19),2805
合成路线图解说明:

The acylation of 4-methoxyaniline (I) with pivaloyl chloride (II) and TEA in CH2Cl2 gives the anilide (III), which is condensed with ethyl trifluoroacetate (IV) by means of n-BuLi in THF yielding the trifluoroacetyl derivative (V). The hydrolysis of the amido group of (V) with 6N HCl in refluxing DMF affords the 2-aminoacetophenone (VI), which is condensed with cyclopropylacetylene (VII) by means of n-BuLi in THF to give the tertiary alcohol (VIII). Finally, this compound is cyclized with phosgene and DIPEA in toluene yielding the racemic form of target compound.

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