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Synthesis of the Hydrazinyl Pyridine Intermediate: Phase-Appropriate Delivery
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2017-08-16 00:00:00 , DOI: 10.1021/acs.oprd.7b00172 Ashraf Wilsily 1 , Steven M. Mennen 1 , Andrew Cosbie 2 , Jacqueline E. Milne 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2017-08-16 00:00:00 , DOI: 10.1021/acs.oprd.7b00172 Ashraf Wilsily 1 , Steven M. Mennen 1 , Andrew Cosbie 2 , Jacqueline E. Milne 1
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A two-step synthesis of an intermediate for a drug-candidate, 3-fluoro-2-hydrazinyl-5-(1-methyl-1H-pyrazol-4-yl)pyridine (1), was developed and optimized according to the strategic priorities of the program. The bond disconnection remained unchanged from the initial route to the scale-up routes; however, the process evolved as the program’s priorities progressed. Speed, securing the raw material supply chain, and cost were all factors considered during development. The strategies to enable multikilogram deliveries are highlighted in this report.
中文翻译：
肼基吡啶吡啶中间体的合成：相适当的传递。
根据该方法开发并优化了两步合成药物候选物的中间体，即3-氟-2-肼基-5-（1-甲基-1 H-吡唑-4-基）吡啶（1）。该计划的战略重点。从初始路线到放大路线，键断开的连接保持不变；但是，随着计划优先级的提高，该过程也在不断发展。速度，确保原材料供应链的安全性和成本是开发过程中考虑的所有因素。本报告重点介绍了实现多千克交付的策略。
更新日期：2017-08-16
中文翻译：
肼基吡啶吡啶中间体的合成：相适当的传递。
根据该方法开发并优化了两步合成药物候选物的中间体，即3-氟-2-肼基-5-（1-甲基-1 H-吡唑-4-基）吡啶（1）。该计划的战略重点。从初始路线到放大路线，键断开的连接保持不变；但是，随着计划优先级的提高，该过程也在不断发展。速度，确保原材料供应链的安全性和成本是开发过程中考虑的所有因素。本报告重点介绍了实现多千克交付的策略。
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