A procedure for the preparation of optically active (2R,5S)- and (2S,5S)-2- Carboxy-l,4-diaza-[4.3.0]bicyclononane is described. The method is based on the reduction of diketopiperazines obtained from cyclization of Pro-L-Ser or Pro-D-Set and occurs without loss of enantiomedc purity. The synthesis is based on readily available starting materials and can be easily arranged for multigram scale preparations.
Synthesis of (2R,5S)- and (2S, SS)-2-Carboxy-l,4-diaza- [4.3.0]bicyclononane as Building Blocks for the Synthesis of New Potential HIV Protease Inhibitors / Porcheddu, Andrea; Giacomelli, G; Falorni, M.. - In: TETRAHEDRON-ASYMMETRY. - ISSN 0957-4166. - 7:7(1996), pp. 1999-2005. [10.1016/0957-4166(96)00241-8]
Synthesis of (2R,5S)- and (2S, SS)-2-Carboxy-l,4-diaza- [4.3.0]bicyclononane as Building Blocks for the Synthesis of New Potential HIV Protease Inhibitors.
PORCHEDDU, Andrea;
1996-01-01
Abstract
A procedure for the preparation of optically active (2R,5S)- and (2S,5S)-2- Carboxy-l,4-diaza-[4.3.0]bicyclononane is described. The method is based on the reduction of diketopiperazines obtained from cyclization of Pro-L-Ser or Pro-D-Set and occurs without loss of enantiomedc purity. The synthesis is based on readily available starting materials and can be easily arranged for multigram scale preparations.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.