Methods and intermediates for the preparation of oligomers containing diastereomerically enriched phosphorothioate linkages are disclosed.
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1. An oligomeric compound comprising a moiety having a phosphate linkage of the Formula XXX: wherein: R3is hydrogen, alkyl, cyanomethyl, monohalomethyl, dihalomethyl, trihalomethyl, --CH2Si(R4)3,or --CH2--SOkR4where k is 0, 1 or 2; R4is independently alkyl, aryl, aralkyl or alkaryl having up t
1. An oligomeric compound comprising a moiety having a phosphate linkage of the Formula XXX: wherein: R3is hydrogen, alkyl, cyanomethyl, monohalomethyl, dihalomethyl, trihalomethyl, --CH2Si(R4)3,or --CH2--SOkR4where k is 0, 1 or 2; R4is independently alkyl, aryl, aralkyl or alkaryl having up to 15 carbon atoms; R5is H, --CN, --Si(R4)3,SOkR4or halogen; or R8and R16are each H, and R3and R5,together, form one of the structures wherein: R10and R11are H, alkyl having from 1 to about 10 carbons, --CH2C(=O)OR22,--CH2CN, --CH2Si(CH3)3,or o- or p-C6H4--R21; R21is hydrogen, --O--C(=O)CH3,alkoxy having from 1 to about 10 carbons, --NO2,or --N(R22)2; R22is independently H or alkyl having from one to about 10 carbon atoms; p is 1 or 2; Z1and Z2are independently halogen, CN, --Si(CH3)3,and --C(=O)OR22; R30is hydrogen, --O--C(=O)CH3,alkoxy having from 1 to about 10 carbons, or --O--Si(R4)3; R6is H, alkyl or aralkyl having up to 15 carbon atoms; or R5and R6,together with the atoms to which they are attached, form a 5 or 6 membered ring; R7is alkyl or aralkyl having up to 15 carbon atoms; or R6and R7,together, form one of the structures wherein X, T, and Z are independently CH or NH; or Z and R5,together with the atoms to which they are attached, form a phenyl ring; R8is H or methyl; R9is a hydroxyl protecting group or a solid support; R16is H, alkyl or aralkyl having up to 15 carbon atoms; B is a nucleobase; and n is an integer from 0 to 50. 2. The oligomeric compound of claim 1 wherein 75% of said phosphosphite linkage is in a single stereoisomeric form.
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이 특허에 인용된 특허 (10)
Stec Wojciech J. (Lodz PLX) Grajkowski Andrzej (Lodz PLX) Uznanski Bogdan (Lodz PLX), Method of making oligonucleotides and oligonucleotide analogs using phospholanes and enantiomerically resolved phosphola.
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