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Updated: May 19, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Mechanistic study of the spiroindolones: a new class of antimalarials
Bin Zou1, Peiling Yap, Louis-Sebastian Sonntag
1Novartis Institute for Tropical Diseases, 10 Biopolis Road, #05-01 Chromos, Singapore. bin.zou@novartis.com
Abstract:
During the synthesis of the new antimalarial drug candidate NITD609, a high degree of diastereoselectivity was observed in the Pictet-Spengler reaction. By isolating both the 4E and 4Z imine intermediates, a systematic mechanistic study of the reaction under both kinetic and thermodynamic conditions was conducted. This study provides insight into the source of the diastereoselectivity for this important class of compounds.
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