PROCESS FOR DEBLOCKING THE 2'-HYDROXYL GROUPS OF RIBONUCLEOSIDES

Title:

PROCESS FOR DEBLOCKING THE 2'-HYDROXYL GROUPS OF RIBONUCLEOSIDES

Document Type and Number:

WIPO Patent Application WO/2006/095739

Kind Code:

A1

Abstract:

A process for deblocking the 2'-hydroxyl groups of ribonucleosides, characterized by reacting a ribonucleoside derivative represented by the general formula (I) wherein the 2'-hydroxyl group is blocked: [Chemical formula 1] (I) [wherein X is hydrogen or the like; Y is hydrogen or the like; and B is a nucleic acid base residue] with a fluorine-containing compound or a basic compound to convert the derivative into a ribonucleoside represented by the general formula (II) or the like: [Chemical formula 2] (II) [wherein X, Y and B are each as defined above].

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Inventors:

SEKINE MITSUO (JP)
SANEYOSHI HISAO (JP)
SEIO KOHJI (JP)

Application Number:

PCT/JP2006/304399

Publication Date:

September 14, 2006

Filing Date:

March 07, 2006

Export Citation:

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Assignee:

TOKYO INST TECH (JP)
SEKINE MITSUO (JP)
SANEYOSHI HISAO (JP)
SEIO KOHJI (JP)

International Classes:

C07H19/067

Foreign References:

JP2004503561A	2004-02-05
JPH07126251A	1995-05-16

Other References:

SANEYOSHI H.: "Synthesis and properties of 2'-O-cyanoethylated RNA derivatives", NUCLEIC ACIDS SYMPOSIUM SERIES, vol. 48, 2004, pages 13 - 14, XP003005809
UMEMOTO T.: "Oligoribonucleotide synthesis by the use of 1-(2-cyanoethoxy)ethyl (CEE) as a 2'-hydroxy protecting group", TETRAHEDRON LETTERS, vol. 45, no. 52, 2004, pages 9529 - 9531, XP004658941
OGILVIE K.K. ET AL.: "A facile method for the removal of phosphate protecting groups in nucleotide synthesis", TETRAHEDRON LETTERS, no. 16, 1976, pages 1255 - 1256, XP003005810
KITA Y. ET AL.: "Protecting group for carboxyl function: mild and facile cleavage of 2-cyanoethyl ester under non-hydrolytic conditions", CHEMICAL PHARMACEUTICAL BULLETIN, vol. 42, no. 1, 1994, pages 147 - 150, XP003005811

Attorney, Agent or Firm:

Nomura, Kenichi (30-1 Tsuruyacho 3-chome, Kanagawa-k, Yokohama-shi Kanagawa 35, JP)

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