Alternative Synthesis of 5‐(1H‐Pyrazol‐4‐yl)‐2‐{6‐[(2,2,6,6‐tetramethylpiperidin‐4‐yl)oxy]pyridazin‐3‐yl}phenol.

Autor:	Zhou, Jianguang, Gu, Xingxian, Yao, Shuping, Ye, Jiong, Fu, Peng, Liu, Siqian, Dedic, Darija, Gallou, Fabrice
Zdroj:	Helvetica Chimica Acta; Mar2023, Vol. 106 Issue 3, p1-12, 12p
Abstrakt:	A scalable and environmentally benign route to the free base of branaplam, a small molecule splicing modulator, was identified and developed. This alternative approach circumvented the inherent risk of dioxin formation associated with ortho‐halo phenol derivatives present in the previous route. A Friedel–Crafts approach provided a reliable access to the key intermediate, subsequently followed by a Suzuki–Miyaura cross‐coupling. Multiple process aspects of the synthetic approach were evaluated, and a robust process for its large‐scale synthesis was developed and successfully demonstrated. [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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