30-05-2013 дата публикации
Номер: US20130137861A1
A reagent for oligonucleotide synthesis or purification, wherein the reagent has a structure of: 1. A reagent for oligonucleotide synthesis or purification , wherein the reagent has a structure of:{'br': None, 'X—C-L-H\u2003\u2003(Formula A)'}whereinX is a phosphoramidite group, an H-phosphonate group, an acetal group, or an isocyanate;{'sub': a', 'b', 'a', '1', '6', '1', '6', 'b, 'C is a direct bond or a cleavable adaptor wherein the cleavable adaptor is represented by —C-C—, wherein Cis connected to X and is a direct bond, hydrocarbyl, aryl, heteroaryl, cycloalkyl, heterocyclyl, a nucleoside, each of which is optionally substituted with one to two substituents selected from halo, hydroxyl, (C-C) alkoxy, (C-C) alkyl, amino or alklyamino; Cis a direct bond, a silanyl group, a trityl group, or a vicinyl alcohol group;'}{'sub': 6', '12', '1', '6, 'L is a hydrocarbyl chain which may be optionally substituted with one to four substituent groups independently selected from the group consisting of 5-to 9-membered heteroaryl, 4- to 9-membered heterocyclyl, amino, ether, carboxyl, carbamoyl, (C-C)aryl, —O—R″, —O—CO—R″, —NR′—R″, —NR′-CO—R″, —CO—NR′R″, —CO—R″, —CN, halogen, or a combination thereof, wherein R′ and R″ are independently H or (C-C)hydrocarbyl; or'}{'sub': a', 'b', 'c', 'd', 'e', '1', '6, 'L is a hydrocarbyl chain interspersed with other atoms, as represented by —(CHR′)—W—(CHR′)—V—(CHR′)—, wherein W and V are independently —O—, —S—, or —NR′—; R′ is H or (C-C)alkyl; and a, b, c, d, and e are independently an integer from 0 to 10; and'}H is a terminal alkyne or an activated cyclooctyne.2. The reagent of claim 1 , wherein H is the activated cyclooctyne group.3. The reagent of claim 1 , wherein C is represented by —C-C— claim 1 , wherein Cis connected to X and is a direct bond claim 1 , (C-C)hydrocarbyl claim 1 , (C-C)aryl claim 1 , 5- to 12-membered heteroaryl claim 1 , (C-C)cycloalkyl claim 1 , 4- to 12-membered heterocyclyl claim 1 , a nucleoside claim 1 , each of ...
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