Phosphitylation process

Details Phosphitylation process Phosphitylation process

C - Chemistry, Metallurgy

07

H

C07H 19/06 (2006.01) C07F 9/24 (2006.01) C07H 19/16 (2006.01)

Patent

CA 2501565

A process for the phosphitylation of an alcohol or thiol with a phosphitylation agent in the presence of an activator is provided. The activator has the formula (1): wherein p is 0 or an integer from 1 to 4 and R for each occurrence is a substituent. Preferably X7 is O and p is 0. The activator is commonly employed as a salt complex with an organic base. Preferred alcohols or thiols include nucleosides and oligonucleotides. The process is particularly suited for the synthesis of phosphoramidites.

L'invention concerne un procédé destiné à la phosphitylation d'un alcool ou d'un thiol avec un agent de phosphitylation en présence d'un activateur. Cet activateur est représenté par la formule générale (1) dans laquelle p vaut 0 ou désigne un entier compris entre 1 et 4 et R désigne un substituant. De préférence, X?7¿ désigne O et p vaut 0. L'activateur est généralement utilisé comme un complexe de sel avec une base organique. Les alcools et les thiols préférés comprennent des nucléosides et des oligonucléotides. Le procédé est particulièrement adapté pour la synthèse de phosphoramidites.

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