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A Facile Synthesis of Raltegravir Potassium—An HIV Integrase Inhibitor
Journal of Heterocyclic Chemistry, 2019A facile, cost‐effective, and commercially viable synthesis of Raltegravir Potassium (1) has been developed from 2‐(1‐amino‐1‐methyl‐ethyl)‐N‐[(4‐fluorophenyl)methyl]‐1,6‐dihydro‐5‐hydroxy‐1‐methyl‐6‐oxo‐4‐pyrimidinecarboxamide (9) with high purity and in good yields.
Kishore Karumanchi +5 more
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Organic Process Research & Development, 2012
Multiple sources of anticipated degradation and process impurities of raltegravir potassium drug substance observed during the laboratory optimization and later during its bulk synthesis are described in this article. The impurities were monitored by UPLC, and their structures are tentatively assigned on the basis of fragmentation patterns in LC–MS and
Golak C. Maikap +8 more
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Multiple sources of anticipated degradation and process impurities of raltegravir potassium drug substance observed during the laboratory optimization and later during its bulk synthesis are described in this article. The impurities were monitored by UPLC, and their structures are tentatively assigned on the basis of fragmentation patterns in LC–MS and
Golak C. Maikap +8 more
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Organic Process Research & Development, 2010
A manufacturing route for the synthesis of raltegravir potassium 1 was developed via a thermal rearrangement of amidoxime DMAD adducts 6 to construct the key, highly functionalized hydroxypyrimidin...
David Askin +10 more
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A manufacturing route for the synthesis of raltegravir potassium 1 was developed via a thermal rearrangement of amidoxime DMAD adducts 6 to construct the key, highly functionalized hydroxypyrimidin...
David Askin +10 more
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Crystal structure of raltegravir potassium, C20H20FKN6O5
Powder Diffraction, 2015The crystal structure of the potassium salt of raltegravir has been solved and refined using synchrotron X-ray powder diffraction data, and optimized using density functional techniques. Raltegravir potassium crystallizes in space groupP21/c(#14) witha= 15.610 59(9),b= 8.148 19(3),c= 16.125 97(6) Å,β= 94.1848(5)°,V= 2045.72(1) Å3, andZ= 4.
James A. Kaduk +3 more
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Biowaiver monograph for immediate-release solid oral dosage forms: Raltegravir potassium
Journal of Pharmaceutical SciencesThe present monograph discusses the possibility of BCS-based biowaivers for immediate release pharmaceutical products containing raltegravir potassium, which is used to treat human immunodeficiency virus (HIV) infections. Raltegravir potassium can be assigned to BCS class II or IV since this compound has low solubility and uncertain permeability ...
Atsushi Kambayashi +12 more
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Synthesis of the HIV Integrase Inhibitor Raltegravir Potassium
Synfacts, 2011Y.-L. Zhong, P. J. Pye, G. R. Humphrey
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