| Autor: |
Reuman M; Johnson and Johnson Pharmaceutical Research & Development, L.L.C., 1000 Route 202, Raritan, New Jersey 08869, USA. mreuman@prdus.jnj.com, Beish S, Davis J, Batchelor MJ, Hutchings MC, Moffat DF, Connolly PJ, Russell RK |
| Jazyk: |
angličtina |
| Zdroj: |
The Journal of organic chemistry [J Org Chem] 2008 Feb 01; Vol. 73 (3), pp. 1121-3. Date of Electronic Publication: 2008 Jan 03. |
| DOI: |
10.1021/jo7021372 |
| Abstrakt: |
The preparation of the selective VEGF-R2 kinase inhibitor 10 (JNJ-17029259) is described in which the key precursor, 4-(5-isoxazolyl)benzonitrile, undergoes clean transformation to the corresponding cumylamine derivative with CeCl(3)-MeLi in THF. This high-yielding cerium mediated transformation is robust, reproducible, and readily scalable based on a requirement for the anhydrous CeCl(3) to be milled and subjected to ultrasound treatment prior to addition of methyllithium. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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