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Updated: Jul 14, 2026

Efficient Construction of Drug-like Bispirocyclic Scaffolds Via Organocatalytic Cycloadditions of α-Imino γ-Lactones and Alkylidene Pyrazolones
Published on: February 7, 2019
Highly selective cascade couplings for the syntheses of functionalized piperidinones and bispidines
Feng Xu1, Edward Corley, Jerry A Murry
1Department of Process Research, Merck Research Laboratories, Rahway, NJ 07065, USA. feng_xu@merck.com
Abstract:
Efficient cascade couplings to synthesize functionalized piperidinones 1 and bispidines 2 and 3 have been developed. Simple modifications to the reaction conditions allow for the highly controlled and selective formation of each compound. In addition, the cis isomer of 1 can be selectively obtained under acidic conditions, while the preparation of the corresponding trans isomer can also be readily realized through a base-catalyzed, dynamic crystallization-driven process.
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