Development of a Practical Synthesis of 4-[6-(Morpholinomethyl)-pyridin-3-yl]naphthalen-1-amine, a Key Intermediate for the Synthesis of BIRB 1017, a Potent p38 MAP Kinase Inhibitor

作者：Lu Bruce Z^*; Li Guisheng; Rodriguez Sonia; Liu Jianxu; Eriksson Magnus C; Tan Zhulin; Song Jinhua J; Yee Nathan K; Farina Vittorio; Senanayake Chris H

来源：Synlett, 2013, 24(3): 317-322.

DOI：10.1055/s-0032-1317790

• metalation
• cross-coupling
• tandem reaction
• boron
• magnesium

The development of synthetic routes to 4-[6-(morpholinomethyl)pyridin-3-yl]naphthalen-1-amine, the key intermediate of p38 MAP kinase inhibitor BIRB 1017, via (1) trialkylmagnesium ate complex mediated metalation and borylation followed by Suzuki coupling reactions and (2) pyridine-ring formation from a vinamidinium salt, is described.

• 出版日期2013-2