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Process Development and Scale-Up of PPAR α/γ Dual Agonist Lobeglitazone Sulfate (CKD-501)
A scaleable synthetic route to the potent PPARα/γ dual agonistic agent, lobeglitazone (1), used for the treatment of type-2 diabetes was developed. The synthetic pathway comprises an effective…
Cyanide as a Powerful Catalyst for Facile Preparation of 2-Substituted Benzoxazoles via Aerobic Oxidation
A cyanide-catalyzed synthesis of 2-substituted benzoxazoles from Schiff bases via aerobic oxidation has been developed. The products from various Schiff bases were obtained in high yields in an open…
Synthesis and Evaluation of Benzoquinolinone Derivatives as SARS‐CoV 3CL Protease Inhibitors.
Alkylated benzoquinolines are designed and synthesized at both the sites of the hydroxyl groups and found that the compound 2a showed five times higher inhibiting activity against the 3CLpro compared to the compound 1.
Access to 1-hydroxymethylpyrrolizidines utilizing malate enolate-imine condensation and ring-closing methathesis: synthesis of (-)-croalbinecine.
The ester enolate-imine condensation route to .beta.-lactams
Enantioselective oxidative coupling of methyl 3-hydroxy-2-naphthoate using mono-N-alkylated octahydrobinaphthyl-2,2′-diamine ligand
Enantioselective additions of diethylzinc and diphenylzinc to aldehydes using 2-dialkyl-aminomethyl-2'-hydroxy- 1,1'-binaphthyls.
These binaphthyl-based axially chiral amino alcohols show high enantioselectivity in the addition of organozincs to aromatic and aliphatic aldehydes.
Free Radical Cyclizations in Alkaloid Total Synthesis: (±)-21-Oxogelsemine and (±)-Gelsemine
Total syntheses of (±)-21-oxogelsemine (3) and (±)-gelsemine (1) are described. Free radical cyclizations play important roles in constructing the tricyclic core (40 → 41) and oxindole (93 → 96)…
Organocatalytic Asymmetric Michael Addition of Ketones to α, β-Unsaturated Nitro Compounds
An organic catalyst “(R, R)-1,2-diphenylethylenediamine(DPEN) derivative’’ was devel-oped as a chiral bifunctional organocatalyst and applied for asymmetric Michael additions of aromatic ketones to…