顺其自然：实施选择性乙缩醛脱保护的新型连续工艺

IF 3.1 3区化学 Q2 CHEMISTRY, APPLIED Organic Process Research & Development Pub Date : 2024-07-11 DOI:10.1021/acs.oprd.3c0040110.1021/acs.oprd.3c00401

Adam Clarke*, Heena Panchal*, Jigang Yang, Yunfeng Bai, Yuedong Wu, Jinxu Sun and Zhiyuan Zhou,

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摘要

DB Mesylate 是生产 cEt amidites 的常用中间体，为阿斯利康的寡核苷酸产品组合提供支持。目前的甲磺酸 DB 生产工艺包括八个阶段，其中有三个分离的中间体，该工艺已经非常成熟。本文介绍了如何实施流程工艺，以解决与关键乙缩醛脱保护阶段相关的产量、产率和生产难题。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Going with the Flow: Implementation of a New Continuous Process for a Selective Acetal Deprotection

DB Mesylate is a common intermediate used in the production of cEt amidites, supporting part of AstraZeneca’s oligonucleotide portfolio. The current process to manufacture DB Mesylate includes eight stages with three isolated intermediates and is well understood. This paper covers the implementation of a flow process to resolve the throughput, yield, and manufacturing challenges associated with the key acetal deprotection stage.

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来源期刊

Organic Process Research & Development 化学-应用化学

CiteScore

6.90

自引率

14.70%

发文量

251

审稿时长

2 months

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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