5448-16-8Relevant articles and documents
TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0230; 0231, (2018/03/25)
The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):
Development of a practical synthesis of a p38 kinase inhibitor via a safe and robust amination
Shi, Zhongping,Kiau, Susanne,Lobben, Paul,Hynes Jr., John,Wu, Hong,Parlanti, Luca,Discordia, Robert,Doubleday, Wendel W.,Leftheris, Katerina,Dyckman, Alaric J.,Wrobleski, Stephen T.,Dambalas, Konstantinos,Tummala, Srinivas,Leung, Simon,Lo, Ehrlic
, p. 1618 - 1625 (2013/02/23)
The development of a practical synthesis for a p38 kinase inhibitor is described. The key advances include an improved route to the key intermediate, a substituted pyrrole, and a subsequent animation utilizing O-(4-nitrobenzoyl)- hydroxylamine, which provides a safe, scalable, and robust amination method. The new protocol was successfully demonstrated to generate 1.6 kg of API in seven steps and 26% overall yield.
Pyrrolopyridazine MEK inhibitors
Chen, Zhong,Kim, Soong-Hoon,Barbosa, Stephanie A.,Huynh, Tram,Tortolani, David R.,Leavitt, Kenneth J.,Wei, Donna D.,Manne, Veeraswamy,Ricca, Carolyn S.,Gullo-Brown, Johnni,Poss, Michael A.,Vaccaro, Wayne,Salvati, Mark E.
, p. 628 - 632 (2007/10/03)
The synthesis and SAR of a series of pyrrolopyridazine MEK inhibitors are reported. Optimal activity was achieved by incorporation of a 4-phenoxyaniline substituent at C4 and an acylated amine at C6.