Shuming Wu, Biyue Lin, Shouzhu Liao and Zhongqing Wang*,
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Review of the Patent and Journal Literature: Synthesis and Final Forms of Antifungal Prodrug Isavuconazonium Sulfate
This review provides a comprehensive summary of the synthesis of the second-generation antifungal agent isavuconazole, its water-soluble prodrug, isavuconazonium, and the prodrug side chain. Establishing contiguous stereocenters and forming the thiazole ring pose the most significant challenges in the synthesis of isavuconazole. Current approaches have faced difficulties in balancing effectiveness and scalability. Additionally, the instability of isavuconazonium, incomplete salt form transformation, and requirement for lyophilization greatly limit the large-scale production of isavuconazonium sulfate. Through this review, we hope to inspire future developments that could potentially address these issues.
期刊介绍：
The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.
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