RU2013151977A - КОНЪЮГАТ миРНК И СПОСОБ ЕГО ПОЛУЧЕНИЯ - Google Patents

КОНЪЮГАТ миРНК И СПОСОБ ЕГО ПОЛУЧЕНИЯ Download PDF

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RU2013151977A
RU2013151977A RU2013151977/10A RU2013151977A RU2013151977A RU 2013151977 A RU2013151977 A RU 2013151977A RU 2013151977/10 A RU2013151977/10 A RU 2013151977/10A RU 2013151977 A RU2013151977 A RU 2013151977A RU 2013151977 A RU2013151977 A RU 2013151977A
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compound
structural formula
polyethylene glycol
skp
following structural
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Бо Рам ХАН
Хан Ох ПАРК
Ми Сик ШИН
Сам Йунг ЛИ
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Байонир Корпорейшн
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Abstract

1. Связанная с полиэтиленгликолем твердая подложка, имеющая следующую структуру:,где R представляет собой алкил, алкенил, алкинил, арил, арилалкил, гетероалкил или гетероарил; m представляет собой целое число от 2 до 18; n представляет собой целое число от 5 до 120; и X представляет собой атом водорода, -монометокситритила, 4,4'-диметокситритил или 4,4',4"-триметокситритила.2. Связанная с полиэтиленгликолем твердая подложка по п. 1, где твердая подложка представляет собой стекло с контролируемым размером пор (СКП).3. Связанная с полиэтиленгликолем твердая подложка по п. 2, в которой СКП имеет диаметр от 40 до 180 мкм и размер пор от 500 до 3000 Å.4. Связанная с полиэтиленгликолем твердая подложка по п. 1, в которой связанная с полиэтиленгликолем твердая подложка представляет собой соединение 3'-ПЭГ(полиэтиленгликоль)-СКП, имеющее следующую структурную формулу IV: [Структурная формула IV]5. Способ получения соединения 3'-ПЭГ-СКП, имеющего следующую структурную формулу IV, который предусматривает:1) реакцию СКП с 3-аминопропилтриэтоксисиланом, с образованием соединения длинноцепочечного алкиламина и стекла с контролируемым размером пор (ДЦАА-СКП);2) реакцию полиэтиленгликоля с 4,4'-диметокситритилхлоридом, в которой образуется 2-[бис-(4-диметокситритил)полиэтиленгликоль)];3) реакцию соединения, полученного на стадии (2), с соединением, имеющим следующую формулу 1, с образованием соединения, имеющего следующую структурную формулу I;4) реакцию полученного соединения, имеющего следующую структурную формулу I, с 4-нитрофенилхлорформиатом, с образованием соединения, имеющего следующую структурную формулу II;5) реакцию соединения, имеющего следующую струк

Claims (5)

1. Связанная с полиэтиленгликолем твердая подложка, имеющая следующую структуру:
Figure 00000001
,
где R представляет собой алкил, алкенил, алкинил, арил, арилалкил, гетероалкил или гетероарил; m представляет собой целое число от 2 до 18; n представляет собой целое число от 5 до 120; и X представляет собой атом водорода, -монометокситритила, 4,4'-диметокситритил или 4,4',4"-триметокситритила.
2. Связанная с полиэтиленгликолем твердая подложка по п. 1, где твердая подложка представляет собой стекло с контролируемым размером пор (СКП).
3. Связанная с полиэтиленгликолем твердая подложка по п. 2, в которой СКП имеет диаметр от 40 до 180 мкм и размер пор от 500 до 3000 Å.
4. Связанная с полиэтиленгликолем твердая подложка по п. 1, в которой связанная с полиэтиленгликолем твердая подложка представляет собой соединение 3'-ПЭГ(полиэтиленгликоль)-СКП, имеющее следующую структурную формулу IV: [Структурная формула IV]
Figure 00000002
5. Способ получения соединения 3'-ПЭГ-СКП, имеющего следующую структурную формулу IV, который предусматривает:
1) реакцию СКП с 3-аминопропилтриэтоксисиланом, с образованием соединения длинноцепочечного алкиламина и стекла с контролируемым размером пор (ДЦАА-СКП);
2) реакцию полиэтиленгликоля с 4,4'-диметокситритилхлоридом, в которой образуется 2-[бис-(4-диметокситритил)полиэтиленгликоль)];
3) реакцию соединения, полученного на стадии (2), с соединением, имеющим следующую формулу 1, с образованием соединения, имеющего следующую структурную формулу I;
4) реакцию полученного соединения, имеющего следующую структурную формулу I, с 4-нитрофенилхлорформиатом, с образованием соединения, имеющего следующую структурную формулу II;
5) реакцию соединения, имеющего следующую структурную формулу I и полученного на стадии (3), с N-сукцинимидилтрифторуксусной кислотой, с образованием соединения, имеющего следующую структурную формулу III; и
6) реакцию соединения ДЦАА-СКП, полученного на стадии (1), с соединениями, имеющими следующие структурные формулы I, II или III, соответственно, и полученными на стадиях (3)-(5), соответственно.
[Формула 1]
Figure 00000003
[Структурная формула I]
Figure 00000004
[Структурная формула II]
Figure 00000005
[Структурная формула III]
Figure 00000006
[Структурная формула IV]
Figure 00000007
(где R представляет собой алкил, алкенил, алкинил, арил, арилалкил, гетероалкил или гетероарил; и n представляет собой целое число, составляющее не менее чем 5 и не более чем 120).
RU2013151977/10A 2009-05-14 2013-11-21 Конъюгат мирнк и способ его получения RU2571218C2 (ru)

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