ВЕРДИН Грегори Л. (US),МИНА Мина (US),ИВАНОТО Наоки (US),БАТЛЕР Дэвид Чарльз Доннелл (US)
申请号：
RU2014105311/04
公开号：
RU2014105311A
申请日:
2012.07.13
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
1. A process for producing phosphorothiotriethers of structure IIIa, comprising the steps of: i) reacting the H-phosphonate of structure Ia with a silylating reagent to provide silyloxyphosphonate； and ii) reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa to provide a phosphorothiotriether of structure IIIa； where the H-phosphonate of structure Ia has the following structure: where W is independently selected from O, S, NH or CH； R is —OH, —SH, —NRR, - N, halogen, hydrogen, alkyl, alkenyl, alkynyl, alkyl-Y-, alkenyl-Y-, alkynyl-Y-, aryl-Y-, heteroaryl-Y-, -P (O) (R), -HP (O ) (R), —OR or —SR； Y is O, NR, S or Se； R is a blocking group； R is a blocking group； each of R is independently hydrogen, alkyl, alkenyl, alkynyl, aryl, acyl, s substituted silyl, carbamate, -P (O) (R) or -HP (O) (R)； each of R is independently hydrogen, alkyl, aryl, alkenyl, alkynyl, alkyl-Y-, alkenyl-Y-, alkynyl-Y -, aryl-Y- or heteroaryl-Y- or a cation which is Na, Li or K； Y is O, NR or S； each of R is independently hydrogen, —OH, —SH, —NRR, —N, halogen, alkyl, alkenyl , alkynyl, alkyl-Y-, alkenyl-Y-, alkynyl-Y-, aryl-Y-, heteroaryl-Y-, -OR or -SR and R is a blocking group； each of Ba is independently blocked or unblocked adenine, cytosine, guanine, thymine, uracil or m difitsirovannym nucleobase； Ryavlyaetsya hydrogen, a protecting group, a linker moiety bound to the solid support or a linker moiety bound to the nucleic acid； and n is from 1 to about 200； the thiosulfonate reagent of structure IIa has the following structure: wherein X is alkyl, cycloalkyl or heteroaryl； R is alk1. Процесс получения фосфоротиотриэфиров структуры IIIa, включающий этапы:i) реагирование Н-фосфоната структуры Iа с силилирующим реагентом для обеспечения силилоксифосфоната； иii) реагирование силилоксифосфоната с тиосульфонатным реагентом структуры IIa для обеспечения фосфоротиотриэфира структуры IIIa；где Н-фосфонат структуры Ia имеет следующую структуру:где W является независимо выбра
