AN EFFICIENT SYNTHESIS OF RADICININ ANALOGS

We describe herein an enantio- and diastereoselective total synthesis of two radicinin analogues 13 and 14. 13 has been subjected to biologi cal tests, exhibiting the lowest toxicity of all radicinin analogues t hat have been investigated to date and it depresses the heart ventricu lar strip and histamine contraction, The key reaction to establish the radicinin skeleton is the reduction of the pseudo C-2 symmetrical pre cursor 11 with the aid of TiCl4 and LiBH4.