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Selective enzymatic hydrolysis of C-terminal tert-butyl esters of peptides

机译:肽C-末端叔丁基酯的选择性酶水解

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In the chemical synthesis of peptides, either a completely linear approach or a convergent approach may be followed. The latter approach, in which the final peptide is assembled from protected peptide fragments, is generally preferred for longer peptides, since overall yields are intrinsically higher and fragments may be prepared in parallel resulting in a shorter overall synthesis time. In a convergent synthesis, all fragments but the C-terminal fragment must be protected at their C-terminal with a protecting function that can be selectively cleaved. In case of peptide synthesis on a solid support, a handle on the support itself usually provides this function. However, for peptide synthesis on a manufacturing scale, solution-phase synthesis is preferred over solid-phase synthesis. Particularly preferred is a synthesis according to DioRaSSP~R, a solution-phase method which combines the advantages of the solid-phase and the classical solution-phase process [1].
机译:在肽的化学合成中,可以遵循完全线性的方法或收敛方法。后一种方法,其中最终肽由受保护的肽片段组装,通常优选用于较长的肽,因为总收率是本质上更高的,并且可以并联制备片段,导致较短的整体合成时间。在收敛合成中,所有片段但必须在其C末端保护C末端片段,其具有可以选择性地切割的保护功能。在固体载体上的肽合成的情况下,支撑件本身上的手柄通常提供该功能。然而,对于制造规模的肽合成,优选在固相合成上优选溶液相合成。特别优选的是根据DiorAssp〜R的合成,一种结合固相和经典溶液相处理的优点的溶液相方法[1]。

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