CHIMIA International Journal for Chemistry · 1996 · 51 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyDrug DesignDrug DiscoverySynthetic Medicinal ChemistryAntiretroviral TherapyAntiviral PharmacologyEnzyme InhibitionOrganic SynthesisProcess SynthesisStereochemical OptimizationAntiviral Drug DesignComplex Molecule SynthesisComplex Organic Molecule FormationMulti-step Synthesis
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.