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    • 5. 发明申请
    • SULFURIZATION REAGENTS ON SOLID SUPPORTS
    • 硫化试剂固体支持
    • US20140179875A1
    • 2014-06-26
    • US14235852
    • 2012-07-24
    • Wieslaw Adam MazurVictor SorokinSteven Karl Laughlin
    • Wieslaw Adam MazurVictor SorokinSteven Karl Laughlin
    • C08F112/08C07H21/04
    • C08F112/08C07B2200/11C07C381/00C07H21/04C12N15/111C12N2310/315C12N2330/30
    • Described herein are novel solid-supported sulfurization reagents having the general structure: (I) wherein (P) is a polymer; X is a linker; R1 is an alkyl group, a cycloalkyl group, an aryl group, or a heterocycle; and R2 is an alkyl group, an aryl group, a methyleneacyloxy group having the formula —CH2—O—C(O)—R7, a methylene carbonate group having the formula —CH2—O—C(O)—OR8, or a methylene carbamate group having the formula —CH2—O—C(O)—NR9R10, wherein R7 is a C1 to C20 hydrocarbon residue, R8 is any alkyl, cycloalkyl, aryl, or heteroaryl, and R9 and R10 are independently hydrogen, alkyl, cycloalkyl, aryl, or heteroaryl. Other embodiments include solid-supported sulfurization reagents having the structure of Formula I, wherein (P) is a polystyrene-based solid support and X is an aromatic linker. Also described herein are methods for synthesizing the solid-supported sulfurization reagents and their use during the synthesis of oligonucleotides.
    • 本文描述了具有以下一般结构的新型固体负载型硫化剂:(I)其中(P)是聚合物; X是一个连接子; R1是烷基,环烷基,芳基或杂环; R2为烷基,芳基,具有式-CH2-O-C(O)-R7的亚甲基酰氧基,具有式-CH2-O-C(O)-OR8的亚甲基碳酸酯基,或 具有式-CH 2 -O-C(O)-NR 9 R 10的亚甲基氨基甲酸酯基,其中R 7为C 1至C 20烃残基,R 8为任何烷基,环烷基,芳基或杂芳基,R 9和R 10独立地为氢,烷基, 环烷基,芳基或杂芳基。 其它实施方案包括具有式I结构的固体支持的硫化试剂,其中(P)是基于聚苯乙烯的固体支持物,X是芳族连接体。 本文还描述了合成固体负载型硫化试剂的方法及其在寡核苷酸合成过程中的用途。