发明名称 Linker arm for solid support oligonucleotide synthesis and process for production thereof
摘要 PCT No. PCT/CA96/00837 Sec. 371 Date Jun. 19, 1998 Sec. 102(e) Date Jun. 19, 1998 PCT Filed Dec. 13, 1996 PCT Pub. No. WO97/23497 PCT Pub. Date Jul. 3, 1997A linker arm for solid support oligonucleotide synthesis, the linker arm comprising formula (1), wherein: X1 is selected from the group consisting of -O-, -S-, -S(O)2-, -C(O)- and -N(R12)-; R12 is selected from the group comprising hydrogen, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkaryl group, X3 is -O- or -N(H)-; R1, R2, R3, R4 and R5 are the same or different and are selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group; n is 0, 1 or 2; and one of A' and B' is selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group, and the other of A' and B' has formula (2), wherein X2 is selected from the group consisting of -O-, -S-, -S(O)2- and -N(R13)-; R13 is selected from the group comprising hydrogen, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkaryl group; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group; p is 0 or 1; and m is 0, 1 or 2. A process for producing the linker arm is also disclosed. The linker arm is useful in solid support oligonucleotide synthesis and is characterized by a desirable combination of stability against spontaneous hydrolysis and ease of intentional cleavage of the synthesized oligonucleotide from the linker arm.
申请公布号 US6015895(A) 申请公布日期 2000.01.18
申请号 US19980091513 申请日期 1998.06.19
申请人 UNIVERSITY TECHNOLOGIES INTERNATIONAL INC. 发明人 PON, RICHARD T.;YU, SHUYUAN
分类号 C07B61/00;C07H19/06;C07H21/00;G01N33/53;G01N37/00;(IPC1-7):C07H21/00;C07H21/02;C07H21/04 主分类号 C07B61/00
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