|
|||||
|
|
A facile synthetic route for antineoplastic drug GDC-0449 |
|
| Authors: | Meng Cao Hua-You Hu Hu-Cheng Zhao Xi-Quan Zhang Hong-Mei Gu Ling Yang Jin Cai Peng Wang Bing Hu Min Ji |
| Affiliation: | 1. School of Biological Science & Medical Engineering, Southeast University, Nanjing, 210096, China 2. Jiangsu Key Laboratory for Chemistry of Low-Dimensional Materials, School of Chemistry and Chemical Engineering, Huaiyin Normal University, Huaian, 223300, China 3. School of Chemistry & Chemical Engineering, Southeast University, Nanjing, 210096, China 4. Nanjing Chia-tai Tianqing Pharmaceutical Co. Ltd., No. 9 Huiou Rd., Economic Development Zone, Nanjing, 210038, China |
| Abstract: | In the current study a facile synthetic route for preparing antineoplastic drug GDC-0449 is investigated. Starting with pyridine-1-oxide and 1-iodo-3-nitrobenzene, the intermediate product 2-(2-chloro-5-nitrophenyl) pyridine was prepared by cross-coupling, deoxidation and halogenation. The final compound was then synthesised by reduction of the nitro group followed by amidation. This synthetic route avoids the use of unstable organometallic or organic boride compounds; it employs relatively inexpensive and bench-stable reagents, involves readily controllable reaction conditions, and achieves a relatively high yield. |
| Keywords: | |
| 本文献已被 SpringerLink 等数据库收录！ | |