Chemical phosphorylation of oligonucleotides and reactants used

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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435 6, 536 221, 536 253, 536 2531, 536 2533, 536 2534, C12Q 168, C07H 1900, C07H 2102, C07H 2100

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059590904

ABSTRACT:
Phosphoramidite building blocks according to the following formula 1 are used for phosphorylating oligonucleotides, preferably at the 5'- or 3'-terminus. The building blocks include phosphoramidite compounds according to formula 1: ##STR1## wherein DMTr is a 4,4'-dimethoxytrityl group; R.sub.1 is an electron withdrawing group; R.sub.2 is an electron withdrawing group which may be the same or different from the R.sub.1 group; R.sub.3 is an alkyl group; and R.sub.4 is an alkyl group which may be the same or different from the R.sub.3 group. Preferred electron withdrawing groups include --CO.sub.2 Et groups, --CO.sub.2 Me groups, --CN groups, --CON(Me).sub.2 groups, and --CONHMe groups, wherein Et represents an ethyl group and Me represents a methyl group. One preferred alkyl group is an isopropyl group.

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