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The presentation contains two parts. The first part showcases our efforts in developing an enantioselective route for the efficient production of complex drug substance (DS) on large scale.聽 The process features an efficient construction of a sterically hindered multi-heterocyclic API with two chiral centers via Hantzsch reaction, highly asymmetric hydrogenation of a ketone, lactone formation, and asymmetric reduction of a hemiketal influenced by the substrate鈥檚 intrinsic chirality.
The second part focusses on research toward a practical method for asymmetric synthesis of P-stereogenic chiral phosphine oxides as key starting materials for synthesis of P-stereogenic phosphine ligand catalysts.