CAS: 17791-51-4; N(α), N-(Im)-Di-Boc-L-Histidine Methyl Ester

相似化合物

7389-87-9 5619-10-3 32946-56-8

上下游产品

CAS号24424-99-5 二碳酸二叔丁酯 | CAS号4467-54-3 D-组氨酸甲酯二盐酸盐 | CAS号71-00-1 L-组氨酸 | CAS号1499-46-3 methyl (2S)-2-a... | CAS号2002-22-4 2-硫代组氨酸

📜L-组氨酸置于氯化亚砜,三乙胺体系中,化学反应 40.0H,反应生成4-((S)-2-叔-丁氧基羰基氨基-2-甲酯基
参考文献:N(π)-2-萘甲氧基甲基保护的组氨酸:肽合成的可扩展,无消旋结构单元
标题:N(π)-2-萘甲氧基甲基保护的组氨酸:肽合成的可扩展,无消旋结构单元
摘要:组氨酸(his)在肽合成过程中相对容易消旋.抑制该消旋作用的一种策略是用合适的保护基保护his中咪唑部分的氮原子.在已经测试的众多保护基团中,π-氮原子上的对甲氧基苄氧基甲基(pmbom)基团有效地抑制了消旋作用.然而,迄今为止,由于需要新鲜制备的不稳定试剂,阻碍了n(π)-Pmbom-保护的衍生物的大规模合成.在此我们报告n的合成(π)-2-萘甲氧基甲基(napom)-保护的his衍生物,其可以克量级制备并且不遭受上述不稳定性问题.此外,这些napom保护的his衍生物可抑制基于boc和fmoc的肽合成中的外消旋作用.
Doi:10.1021/acs.Oprd.9B00538

专利信息

专利号:US-10266565-B2
优先权日:2011-04-12
标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN
权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.

专利号:US-4591648-A
优先权日:1981-04-01
标 题:Histidine protection
发明人：JONES JOHN H; BROWN TOM
权利人:NAT RES DEV
摘要:Histidine derivatives of formula I are useful inter alia in peptide synthesis. ##STR1## wherein: X represents --CH 2 OCH 2 Ar, in which Ar is a phenyl substituent optionally substituted by one or more halogen, alkoxy, alkyl or nitro groups; n Y, which differs from X, represents hydrogen, a protective group capable of inhibiting self coupling during formation of a peptide bond, an amino acid residue, a peptide chain or an antibiotic residue; n E represents OH,OM,M representing an alkali metal or ammonium, OR, R representing an alkyl, aryl, aralkyl or alkaryl group, an amino acid residue, a peptide chain or an antibiotic residue; n the compound I being optionally in the form of a hydrate or acid salt. n In compounds I of especial interest, X represents benzyloxymethyl or p-bromobenzyloxymethyl, Y represents t-butyloxycarbonyl and E represents --OH.