CAS: 18534-18-4; Phosphoric Acid,Piperazine,Hydrate

专利信息

专利号:US-6632942-B2
优先权日:2000-05-04
标题:Asymmetric synthesis of piperazic acid and derivatives thereof
发明人：ROBIDOUX ANDREA L C; SERAFINI SIRO; DIETERICH PETRA; LEONARDI STEFANIA; STIBBARD JOHN
权利人:VERTEX PHARMA
摘要:This invention provides a concise, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2,5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups, such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.

专利号:US-2003176691-A1
优先权日:2000-05-04
标 题:Asymmetric synthesis of piperazic acid and derivatives thereof

专利号:EP-1280780-A2
优先权日:2000-05-04
标 题:Asymmetric synthesis of piperazic acid and derivatives thereof

专利号:EP-1280780-B1
优先权日:2000-05-04
标题:Asymmetric synthesis of piperazic acid and derivatives thereof

专利号:WO-0183458-A2
优先权日:2000-05-04
标 题:Asymmetric synthesis of piperazic acid and derivatives thereof