Novel C-4 heteroaromatic kainoid analogues: a parallel synthesis approach |
| |
| Authors: | Baldwin J E Fryer A M Pritchard G J |
| |
| Affiliation: | The Dyson Perrins Laboratory, Oxford, UK. jack.baldwin@chem.ox.ac.uk |
| |
| Abstract: | New C-4 thiazole 4, 5 and aminothiazole 6, 7 kainoid analogues were efficiently synthesised in five steps from commercially available (-)-alpha-kainic acid I and exhibited strong binding to the kainate receptors. A reactive alpha-bromoketone 10 was generated and reacted with thioamides and thioureas to form thiazole and aminothiazole heterocycles 11-14. Deprotection gave the new kainoid amino acids 4-7 in excellent yield. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
