Synthesis of a Bicyclic Piperazine from l-Aspartic Acid and Application of a Fluoride-Promoted SNAr Coupling

…, JD McKinley, DE Bourassa, JJ Teixeira…

文献索引：Sieser, Janice E.; Singer, Robert A.; McKinley, Jason D.; Bourassa, Dennis E.; Teixeira, John J.; Long, James Organic Process Research and Development, 2011 , vol. 15, # 6 p. 1328 - 1335

全文：HTML全文

被引用次数: 4

摘要

The process development is reported of a pivotal C–N bond formation involving ((7 R, 9a S)- octahydro-1 H-pyrido [1, 2-a] pyrazin-7-yl) methanol (2) undergoing nucleophilic aromatic substitution with 3-chlorobenzo [d] isoxazole (3) to furnish ((7 R, 9a S)-2-(benzo [d] isoxazol- 3-yl) octahydro-1 H-pyrido [1, 2-a] pyrazin-7-yl) methanol (4) as a key intermediate for a family of compounds (1). Essential to the success of the coupling is the use of fluoride in ...