公开(公告)号：WO1984002526A1

公开(公告)日：1984-07-05

申请号：PCT/US1983002056

申请日：1983-12-29

Applicant: SOUTHERN ILLINOIS UNIVERSITY FOUNDATION

Inventor： SOUTHERN ILLINOIS UNIVERSITY FOUNDATION ,  SUNG, Michael, T. ,  CAO, Tin, M. ,  BINGHAM, Scott, E.

IPC: C07H15/12

CPC classification number: C07H21/00

Abstract: In a transverse phosphite process for preparation of polynucleotides, a 5' reactive resin nucloside is reacted with a bifunctional phosphorus (III) reagent to produce a monofunctional resin nucleosidophosphorus (III) intermediate. This intermediate is condensed with a 3' reactive 5' blocked nucleoside to produce a dinucleosidophosphite. The latter is 5' deblocked and the cycle of reaction with bifunctional intermediate and condensation with 5' blocked 3' reactive nucleoside repeated to build a chain corresponding to the desire polynucleotide. Phosphite is converted to phosphate by oxidation to produce the polynucleotide. Improved structures and processes for linking the nucleotide chain to the resin, and improve techniques for detaching the final nucleotide from the resin are also disclosed.

Abstract translation: 在用于制备多核苷酸的亚磷酸亚酯方法中，将5'反应性树脂核苷酸与双功能磷（III）试剂反应以制备单官能树脂核苷酸（III）中间体。 该中间体与3'反应性5'封闭核苷缩合以产生二核苷酸亚磷酸酯。 后者为5'解封端，并与双功能中间体反应循环，并与5'封闭的3'反应性核苷缩合，重复构建对应于所需多核苷酸的链。 通过氧化将亚磷酸酯转化成磷酸盐以产生多核苷酸。 还公开了将核苷酸链与树脂连接的改进的结构和方法，以及用于从树脂中分离最终核苷酸的改进技术。