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Synthesis of the HIV-Proteinase Inhibitor Saquinavir: A Challenge for Process Research
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1996
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Combinatorial ChemistryBioorganic ChemistryMolecular BiologyAntiviral DrugMedicinal ChemistryAntiviral Drug DevelopmentStereoselective SynthesisProcess ResearchHiv-proteinase Inhibitor SaquinavirComplex MoleculeBiochemistryVirologyHivNatural Product SynthesisAntiviral CompoundPharmacologyNatural SciencesAntiviral TherapySynthetic BiologyMedicineDrug Discovery
The task of process research, namely developing efficient, economically and technically as well as ecologically feasible syntheses in time, is demonstrated on the HIV-proteinase inhibitor Saquinavir, a complex molecule comprising six stereo-centres. Based on the first 26-step research synthesis furnishing a 10% overall yield, process research established a new, short 11-step synthesis affording a 50% overall yield.