Paroma Chakravarty*, Jie Xu, Brandon Scott, Sarah J. Robinson and Karthik Nagapudi,
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引用次数: 0
Abstract
Giredestrant (GDC-9545) is a selective estrogen receptor degrader that was developed as a tartrate salt. The first GMP batch was manufactured via a crystallization-driven diastereoselective Pictet–Spengler condensation. This batch underwent an additional rework step due to inherent challenges involving purity, yield, and preservation of the desired polymorphic form. This study outlines the solid-state characterization experiments conducted to identify the appropriate route and solvent composition for the required rework to deliver a drug substance clinical batch with the desired polymorphic form, yield, and purity.
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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