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Process for preparing ([R-(R*,R*)]-2-(4-fluorophenyl)-,-dihydroxy-5-(1-methylethyl)-3 phenyl-4-[(phenylamino)carbonyl]-lH-pyrrole-l-heptanoic acid)

IP.com Disclosure Number: IPCOM000181878D
Publication Date: 2009-Apr-16
Document File: 2 page(s) / 26K

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 Process for preparing ([R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1- methylethyl)-3 phenyl-4-[(phenylamino)carbonyl]-lH-pyrrole-l-heptanoic acid)

    ([R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3 phenyl-4- [(phenylamino)carbonyl]-lH-pyrrole-l-heptanoic acid) (ATV) is depicted in lactone form in the following Formula (I) and its calcium salt trihydrate (ATV hemi-calcium) of the following Formula (II) (water molecules not shown)

    A crystalline ATV hemi-calcium named form VIII, is characterized by a physical or spectroscopic analysis result selected from the group consisting of:
a) a powder X-ray diffraction pattern generated using CuKa radiation with peaks at 9.3,
9.6, 16.3, 19.2 ,20.0 ,21.6 ,22.4 ,23.9 ± 0.2 degrees two-theta;

b) a solid state cross-polarization/magic angle spinning 13C nuclear magnetic resonance spectrum with resonances at 24.8, 25.2, 26.1, 119.5, 120.1, 121.8, 122.8, 126.6, 128.8, 129.2, 134.2, 135.1, 137.0, 138.3 and 139.8 ± 0.1 parts per million; and
c) a solid state cross-polarization/magic angle spinning 13C nuclear magnetic resonance spectrum wherein the chemical shift differences between the lowest resonance and other resonances are: 2.2, 7.0, 7.4, 8.3, 22.5, 23.0, 23.7, 25.6, 26.3, 28.3, 53.0, 55.5, 96.3, 98.2, 101.7, 102.3, 104.0, 105.0, 108.8, 111.0, 111.4, 116.4, 117.3, 119.2, 120.5, 122.0,...