| Autor: |
Garcia-Losada, Pablo, DeBaillie, Amy C., Eugenio de Diego, Jose, Green, Steven J., Hansen, Marvin M., Jaramillo, Carlos, Johnson, Matt, Kaoudi, Talbi, Li, Jiuyuan, Lindsay-Scott, Peter J., Mateos, Carlos, Mergott, Dustin J., Rincon, Juan Antonio, Rothhaar, Roger R., Seibert, Kevin D., Watson, Brian M., Winneroski, Leonard L., Gangula, Srinivas, Jing, Dajiang, Sun, Hao, Zhang, Lei, Frederick, Michael O. |
| Zdroj: |
Organic Process Research & Development; February 2020, Vol. 24 Issue: 2 p306-314, 9p |
| Abstrakt: |
Herein we report a summary of the synthetic development of LY3202626 from the initial discovery route to a final route that was scaled to make 150 kg. Key developments include the use of a [3 + 2] cyclization to set the cis ring junction of the formed isoxazoline, a one-pot thiazine formation, and three different ways to install the aniline: (1) Cu-catalyzed azide coupling and reduction, (2) nitration and reduction, and (3) Buchwald coupling with acetamide. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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