P. Christov, I. Kozekov, M. Palamareva
Jul 1, 2006
Citations
0
Influential Citations
7
Citations
Journal
Journal of Heterocyclic Chemistry
Abstract
The parent compound 5-oxo-10a-phenyl-2,3,10,10a-tetrahydro-5H-[1,3]-oxazolo-[3,2-b]-isoquinoline-10-carboxylic acid (5) was prepared in large scale and a good yield by reaction between homophthalic anhydride (3) and 4,5-dihydro-2-phenyl-1,3-oxazole (4). Thus, the closure of the isoquinoline ring and fusion of the 1,3-oxazol ring occur in one step. Trans configuration was assumed for the product. The parent acid 5 was converted in four steps to the target aminomethyl derivatives 9a-1. The latter contain four features that make them interesting from pharmaceutical point of view.