| 摘要 |
<p>The invention relates to pyrrole derivatives, namely [3-phenyl-4-(phenylcarbamoyl)-2-(4- flu orophenyl)-5-(1-methylethyl)-pyrrol-1-yl] methyl(diphenyl)phosphine oxide (I) and diethyl[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluoropheny1)-5-(1-methylethyl)-pyrrole-1-yl]methylphosphonate (II), and to their preparation. (I) can be synthesised by reacting N-(bromomethyl)phtalimide with ethyl diphenylphosphinite to form diphenyl(phthalimidomethyl)phosphine oxide, subsequently treated with hydrobromic acid to give aminomethyl(diphenyl)phosphine oxide, which can be condensed with an atorvastatin 1,4-diketo compound (VI, Scheme 2) to yield (I). (II) can be prepared by reacting N-(bromomethyl)phtalimide with triethyl phosphite to form diethyl phthalimidomethylphosphonate, subsequently treated with hydrazine hydrate to give diethyl amninophosphonate, which is condensed with atorvasatin 1,4-dicarbonyl compound (VI, Scheme 2) to yield (II). Compounds (I) and (II) may be useful in the synthesis of atarvastatin.</p> |
