Phosphitylation process

Details Phosphitylation process Phosphitylation process

2007-07-24

2007-07-24

Saeed, Kamal A. (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

C536S026100, C548S206000

Reexamination Certificate

active

10531323

ABSTRACT:
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:wherein p is 0 or an integer from 1 to 4 and R for each occurrence is a substituent. Preferably X7is 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.

REFERENCES:
patent: 5034534 (1991-07-01), Milstein
patent: 6275725 (2001-08-01), Cosman
patent: WO 03/4512 (2003-01-01), None
Sanghvi et al., “Improved process fro the preparation of nucleosidic phosphoramidites using a safer and cheaper activator”, Organic Process Reaserch & Development, 2000, pp. 175-181, No. 3, American Chemical Society.

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