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Automatic system for the synthesis and chemical modification of oligomers having a predetermined sequence using soluble supporting polymers

机译:使用可溶性支持聚合物合成和化学修饰具有预定序列的低聚物的自动系统

摘要

The synthesis of oligomers in a predetermined sequence, such as peptides, oligosaccharides, oligonucleotides, etc., is very important in the sectors using those products for diagnostic and therapeutic use. The problem of their synthesis has now been solved through the use of insoluble supporting polymers which aid intermediate purification and automation of the corresponding synthesis process. The polymer in fact makes it possible to convert the intermediate purification processes into simple filtrations and washes. These systems, even though they can be automated, are of limited application for large scale production on account of the heterogeneity of the process and the requirement for large quantities of reagents. This system makes it possible to use soluble polymers which instead permit operation in a homogeneous phase. In this way a lesser quantity of reagents is required for an equal yield and increasing the scale of synthesis is not impeded by the phase heterogeneity of the process, which makes the yield from synthesis unforeseeable and renders it difficult to handle large quantities of support. The use of this system is dedicated to the large scale synthesis of natural and chemically modified oligomers, having a predetermined sequence which may or may not be stably bound to the supporting polymer, carried out using automated processes.
机译:在使用那些产品用于诊断和治疗用途的领域中,以预定顺序合成低聚物,例如肽,寡糖,寡核苷酸等,是非常重要的。现在已经通过使用不溶性支持聚合物解决了它们的合成问题,所述不溶性支持聚合物有助于相应的合成过程的中间纯化和自动化。实际上,该聚合物使得将中间纯化过程转化为简单的过滤和洗涤成为可能。这些系统即使可以自动化,但由于过程的异质性和对大量试剂的需求,在大规模生产中应用有限。该系统使得可以使用可溶的聚合物,其相反地允许在均相中操作。以这种方式,需要较少量的试剂以获得相同的收率,并且该方法的相异质性不会阻碍合成规模的增加,这使得不可预见的合成收率并且使得难以处理大量的载体。该系统的使用专用于天然和化学修饰的低聚物的大规模合成,该低聚物具有使用自动化方法进行的具有预定序列的序列,该预定序列可能或可能不会稳定地结合到支持聚合物上。

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