Development and Scale-Up of an Enabling Synthetic Route to KTX-005, a Muscarinic Acetylcholine Receptor Agonist for the Potential Treatment of Schizophrenia

Development and Scale-Up of an Enabling Synthetic Route to KTX-005, a Muscarinic Acetylcholine Receptor Agonist for the Potential Treatment of Schizophrenia

Hanchao Zheng , Rui Zhang , Michel Leeman , Christopher R. H. Hale , Giorgio Attardo , Vijaya B. Gondi  *

* Email: gondib@gmail.com

 

 

ABSTRACT

 

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.

 

 

 

CAPABILITIES

Library

Targeted Protein Degrader

Flow Chemistry

Reaction Condition Screening

Computer-aided Drug Design

Bio-Transformation

Analysis & Purification

Chemistry Synthesis

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