Three-Step Continuous Flow Synthesis of the Intermediate 4-Fluoro-2-methoxy-5-nitrophenol of Linzagolix DOI

Tengfei Gong,

Fei Ji, Yang Shi

et al.

Organic Process Research & Development, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 18, 2024

4-Fluoro-2-methoxy-5-nitrophenol is a key intermediate of the GnRH receptor antagonist Linzagolix. The traditional synthetic methods have several disadvantages including prolonged reaction time and safety issues. Herein, we describe three-step continuous flow synthesis 4-fluoro-2-methoxy-5-nitrophenol via esterification, nitration, hydrolysis. total residence was 234 s, yield 85.6%, which substantially reduced considerably improved process as well yield.

Language: Английский

Industry Perspective on the Selection of Regulatory Starting Materials for Synthetic Peptides DOI
Subha Mukherjee, David A. Thaisrivongs, Paridhi Agrawal

et al.

Organic Process Research & Development, Journal Year: 2025, Volume and Issue: unknown

Published: Feb. 26, 2025

Language: Английский

Citations

0

Chemical Process Development in the Pharmaceutical Industry in Europe—Insights and Perspectives from Industry Scientists DOI Creative Commons
Joachim I. Krueger, André P. Dieskau,

Jorma Hassfeld

et al.

Angewandte Chemie International Edition, Journal Year: 2025, Volume and Issue: unknown

Published: March 27, 2025

Chemical process development is a critical component in the for active pharmaceutical ingredients (APIs). With interfaces to drug discovery and API manufacturing, chemical activities must deliver scalable, safe, cost-efficient, sustainable, reliable processes novel as well marketed APIs. Despite its importance industry society, domain of development, together with advances challenges, often not known nonpractitioners. As scientists, we provide scientific perspective on state affairs which believe will be value broader audience, including academic researchers, students, professionals from related fields.

Language: Английский

Citations

0

Chemical Process Development in the Pharmaceutical Industry in Europe—Insights and Perspectives from Industry Scientists DOI Creative Commons
Joachim I. Krueger, André P. Dieskau,

Jorma Hassfeld

et al.

Angewandte Chemie, Journal Year: 2025, Volume and Issue: unknown

Published: March 27, 2025

Abstract Chemical process development is a critical component in the for active pharmaceutical ingredients (APIs). With interfaces to drug discovery and API manufacturing, chemical activities must deliver scalable, safe, cost‐efficient, sustainable, reliable processes novel as well marketed APIs. Despite its importance industry society, domain of development, together with advances challenges, often not known nonpractitioners. As scientists, we provide scientific perspective on state affairs which believe will be value broader audience, including academic researchers, students, professionals from related fields.

Language: Английский

Citations

0

Recent Advances in the Application of Foodborne Substances in Hyperuricemia DOI
Yanxia Liu, Wei Deng, Fashan Wei

et al.

Journal of Agricultural and Food Chemistry, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 4, 2024

Hyperuricemia (HUA) is a purine metabolism disorder characterized by the excessive production or inadequate excretion of uric acid. Current pharmacological strategies targeting acid reduction have potential adverse effects. Following concept "homology medicine and food", food ingredients are increasingly being explored to prevent HUA gout, with xanthine oxidase (XOD) emerging as crucial therapeutic target in managing HUA. Recent scientific investigations determined that acid-lowering substances come from various sources, such seafood, dairy products, agricultural products. These bioactive attracted wide attention because their effective antihyperuricemia XOD inhibitory ability. In this study, pathogenesis, many side effects drugs, some components drugs mainly described, emphasis on source, composition, preparation technology, mechanism peptides.

Language: Английский

Citations

2

Three-Step Continuous Flow Synthesis of the Intermediate 4-Fluoro-2-methoxy-5-nitrophenol of Linzagolix DOI

Tengfei Gong,

Fei Ji, Yang Shi

et al.

Organic Process Research & Development, Journal Year: 2024, Volume and Issue: unknown

Published: Dec. 18, 2024

4-Fluoro-2-methoxy-5-nitrophenol is a key intermediate of the GnRH receptor antagonist Linzagolix. The traditional synthetic methods have several disadvantages including prolonged reaction time and safety issues. Herein, we describe three-step continuous flow synthesis 4-fluoro-2-methoxy-5-nitrophenol via esterification, nitration, hydrolysis. total residence was 234 s, yield 85.6%, which substantially reduced considerably improved process as well yield.

Language: Английский

Citations

1