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New Compounds useful as intermediaries benzoxazoles devoid of Therapeutic activity for the preparation of pharmaceutically Active benzoxazoles
New Compounds useful as intermediaries benzoxazoles devoid of Therapeutic activity for the preparation of pharmaceutically Active benzoxazoles
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机译:用作中间体的苯并恶唑的新化合物,对制备药物活性的苯并恶唑没有治疗活性
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1490067 2-Phenyl-benzoxazoles LILLY INDUSTRIES Ltd 22 Oct 1974 [23 Oct 1973] 49258/73 Heading C2C Novel 2-phenyl-benzoxazoles of the general formula wherein the -CRSP1/SPRSP2/SPRSP3/SP group is in the 5- or 6- position of the benzoxazole nucleus, RSP4/SP is a phenyl group optionally substituted by at least one C 1-6 alkylsulphonyl, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl, nitro, C 2-7 acyl, hydroxy, amino, C 1-6 alkylamino or C 2-7 acylamino radical or optionally substituted in two adjacent positions by a methylene- or ethylene-dioxy radical, RSP3/SP is a nitrile group, a carboxy group or a salt, ester, amide or hydroxamic acid derivative thereof, or a hydroxymethyl group or an ester thereof, RSP1/SP is a hydrogen atom or a C 1-6 alkyl group and RSP2/SP is a halogen atom or a hydroxy or C 2-7 acyloxy group, are prepared by cyclizing a benzene derivative of the general formula wherein V, W and Z are respectively RSP1/SP, RSP2/SP and RSP3/SP or atoms or groups which are respectively convertible to RSP1/SP, RSP2/SP and RSP3/SP and either X is a hydrogen atom or RSP4/SPCO- and Y is H 2 N- or X is a hydrogen atom and Y is RSP4/SPCONH- or RSP4/SPCH=N-, the cyclization being effected, in the case where X is a hydrogen atom and Y is H 2 N-, in the presence of RSP4/SPCOOH, (RSP4/SPCO) 2 O, RSP4/SPCOOl, RSP4/SPCONH 2 , RSP4/SPCONHNH 2 , RSP4/SPCN, or RSP4/SPCCl=NRSP7/SP (RSP7/SP is C 1-4 alkyl) and thereafter, where one or more of V, W and Z in the product are not the same as RSP1/SP, RSP2/SP and RSP3/SP, respectively, converting V, W and/or Z to RSP1/SP, RSP2/SP and/or RSP3/SP in conventional manner. 2 - p - Chlorophenyl - 6 - benzoxazolylcarboxaldehyde is prepared by brominating 2-pchlorophenyl - 6 - methyl - benzoxazole and oxidizing the resulting 2 - p - chlorophenyl - 6- benzoxazolylmethyl bromide. The novel 2-phenyl-benzoxazoles can be reduced to give the corresponding compounds in which RSP2/SP is a hydrogen atom.
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