CAS: 32750-52-0; Hexahydropyridazine-3-Carboxylic Acid

相似化合物

1219380-72-9 72064-50-7 2738899-29-9

上下游产品

(+/-) hexahydropyridazine-3-carboxylic acid hydr°Chloride N,N'-di-tert-butoxycarbonylpiperazic acid

📜1,2-双(叔丁氧基羰基)六氢哒嗪-3-羧酸置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 4.0H,反应生成 六氢哒嗪-3-羧酸
参考文献:环状α-肼基酸的合成
标题:环状α-肼基酸的合成
摘要:描述了从常见的起始原料"丙二酸二乙酯"以26,16,34,13.5和13.33%的总收率合成五元,六元,七元,八元和九元环状α-肼基酸.顺序烯丙基化或均烯丙基化和亲电胺化,然后环化,得到所需的环.通过rcm合成八元环和九元环的甲酯,并在dcm中的1 M Bbr 3溶液存在下水解后反应生成相应的游离酸.
DOI:10.1016/j.Tet.2012.07.014

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-2022372533-A1
优先权日:2017-06-30
标 题 :Transgenic microorganisms and synthesis of piperazic acid, piperazic acid containing products, and derivatives thereof
发明人：VAN DYKE-BLODGETT JOSHUA; HU YIFEI
权利人:VAN DYKE BLODGETT JOSHUA; HU YIFEI; WASHINGTON UNIVERSITY ST LOUIS
摘要:Among the various aspects of the present disclosure is the provision of a biological and biochemical production of piperazic acid derived from the newly discovered production pathway for L-piperazic acid. One aspect of the present disclosure includes a transgenic microorganism (e.g., bacteria) engineered to accumulate piperazic acid and derivatives thereof, including a piperazic acid (Piz)-containing product. Another aspect of the present disclosure includes biochemical and biological methods for producing piperazic acid and derivatives thereof, including a piperazic acid (Piz)-containing product. Another aspect of the present disclosure includes compositions and methods of using isotopically labeled piperazic acid and derivatives thereof, including a piperazic acid (Piz)-containing product.

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:WO-2024216017-A2
优先权日:2023-04-14
标题:Synthesis of ras inhibitors

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:US-2024368190-A1
优先权日:2023-04-14
标题:Synthesis of ras inhibitors
发明人：LI SHAOLING; MANTHATI SURESH; WANG ROSS; BALLMER STEVE; HUANG XIAOJUN
权利人:REVOLUTION MEDICINES INC
摘要:The present invention relates to Ras inhibitors and to methods for preparing Ras inhibitors.