会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明授权
    • Method for reductive elimination of protecting groups
    • 还原消除保护基团的方法
    • US4564471A
    • 1986-01-14
    • US188107
    • 1980-09-17
    • Katsumi SugiyamaHideo TakedaHiroko SatoYuji NonakaKiyotaka OyamaMasashige Kubo
    • Katsumi SugiyamaHideo TakedaHiroko SatoYuji NonakaKiyotaka OyamaMasashige Kubo
    • C07B31/00C07B51/00C07C67/00C07C227/00C07C227/16C07C227/18C07C227/20C07C231/00C07K1/06C07K1/12C07K5/075C07C101/02
    • C07K1/12C07K5/0613Y02P20/55
    • The invention provides a novel and efficient method for the elimination of protecting groups, e.g. benzyloxycarbonyl group, from a protected amino acid, peptide or derivative thereof having at least one functional group protected by a protecting group, e.g. a lower alkyl ester of N-benzyloxycarbonyl-.alpha.-L-aspartyl-L-phenylalanine by catalytic hydrogen reduction to produce free amino acid, peptide or derivative thereof. In contrast to the conventional procedures in which the reaction is carried out in a solvent dissolving both the starting compound and the product compound or a solvent dissolving the starting compound but not dissolving the product compound, the inventive method utilizes a binary two-phase reaction medium composed of water and an organic solvent not freely miscible with water such as toluene. The reaction takes place in the organic phase containing the starting compound dissolved and the catalyst dispersed therein whereas the reaction product which is water-soluble is smoothly and successively transferred into the aqueous phase so that advantages are obtained in the unexpectedly high yield of the product as well as in the easiness of handling the reaction mixture after completion of the reaction.
    • 本发明提供了一种用于消除保护基团的新型和有效的方法,例如, 苄氧羰基,被保护的氨基酸,具有至少一个被保护基保护的官能团的肽或衍生物。 N-苄氧羰基-α-L-天冬氨酰基-L-苯丙氨酸的低级烷基酯通过催化氢还原反应产生游离氨基酸,肽或其衍生物。 与在溶解起始化合物和产物化合物的溶剂或溶解起始化合物但不溶解产物化合物的溶剂中进行反应的常规方法相反,本发明的方法利用二元二相反应介质 由水和不能与水如甲苯自由混溶的有机溶剂组成。 反应发生在含有溶解的起始化合物和分散在其中的催化剂的有机相中,而水溶性的反应产物顺利地依次转移到水相中,从而获得了产品出乎意料的高产率的优点, 以及在反应完成后容易处理反应混合物。