Convenient Route to Efavirenz Analogues as Potential non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors
نویسندگان
چکیده
Treating 2-chloro-4-(4-chlorophenyl)-6-methylbenzo[d]-3,1-oxazinium hexachloroantimonate (1) with one equivalent of alcohol or mercaptane led, after hydrolysis with aq. NaOH, to the formation of 4,4-disubstituted-1,4-dihydro-2H-6-methyl-3,1-benzoxazin-2-ones (3). Large excess addition of alcohol afforded either 4’-chloro-2-isocyanato-5-methylbenzophenone disubstitutedketal (4) or N-{2[(4-chlorophenyl)dialkoxymethyl]-4-methylphenyl} alkylcarbamate (5). Reaction of 4 with primary amines furnished 1-{2-[(4-chlorophenyl)dialkoxymethyl]-4-methylphenyl}-3-substituted urea (6).
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