CAS: 197632-83-0; N-Me-Ser(Tbu)-Oh

相似化合物

128107-47-1 13734-38-8 1676-75-1

上下游产品

O-叔丁基-L-丝氨酸 (S)-O-Tert-Butylserine 18822-58-7

📜聚合甲醛,O-叔丁基-L-丝氨酸置于四氢吡咯体系中,用85 %的收率获得o-叔丁基-N-甲基-L-丝氨酸
参考文献:六氟异丙醇中分子间反应中甲醛介导的烷基胺氢化物释放
标题:六氟异丙醇中分子间反应中甲醛介导的烷基胺氢化物释放
摘要:烷基胺自发释放氢阴离子的能力通常受到限制,除非在特定的分子内反应设置下.在此,我们证明这种反应活性可以通过在六氟异丙醇(hfip)溶剂中用甲醛进行简单处理来释放,从而在温和条件下实现烷基胺的各种分子间氢化物转移反应.除了小分子的转化之外,这些反应还可以对复杂肽进行独特的后期修饰.机理研究发现,这些分子间氢化物转移过程的关键在于溶剂介导的大环过渡态的调节构象,其中 Hfip 分子的聚集体充当灵巧的质子穿梭机.重要的是,氮的孤电子对与胺的αc-H键的反键轨道之间的负超共轭在c-H活化中起着关键作用,促进其氢化物释放.
Doi:10.1021/jacs.3C12215

专利信息

专利号:US-12351573-B2
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; CHENG KAI FAN
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2023159450-A1
优先权日:2020-05-08
标 题 :Dimers for use in synthesis of peptidomimetics
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:WO-2025128985-A1
优先权日:2023-12-14
标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.

专利号:US-11440881-B2
优先权日:2019-05-09
标题 :Thiosemicarbazates and uses thereof
发明人：AL-ABED YOUSEF; ALTITI AHMAD
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

专利号:US-2022372022-A1
优先权日:2019-05-09
标 题:Compounds for use in synthesis of peptidomimetics