WuXi Biologics
Offering End-to-End Solutions
Hanchao Zheng , Rui Zhang , Michel Leeman , Christopher R. H. Hale , Giorgio Attardo , Vijaya B. Gondi *
* Email: gondib@gmail.com
Development and optimization of phase-appropriate synthetic technologies to prepare KTX-005, a potent muscarinic acetylcholine receptor agonist, are described in this article. The modular strategy involves three building blocks: commercially available materials dichlorothiadiazole (21), butanethiol (22), and custom-synthesized azabicyclo derivative (18). The highlight of the enabling synthetic strategy toward KTX-005 is a unique thiadiazole ring opening/closing sequence to facilitate both dichlorothiadiazole desymmetrization with butanethiol as well as functionalization of the azabicyclo ring derivative 18.
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