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Document Type and Number:
WIPO Patent Application WO/2010/150791
Kind Code:
Disclosed is a novel process for the production of an adenosine tetraphosphate, by which an adenosine tetraphosphate can be synthesized more easily in an enhanced yield in comparison with conventional processes. In the novel process, the synthesis of a compound of general formula (I) from a compound of general formula (XI) is conducted by converting a compound of general formula (XI) into the corresponding cyclic triphosphate compound of general formula (XIV) using a carbodiimide as a condensation agent, and then reacting the cyclic triphosphate compound with a compound of general formula (VIII) in the presence of a salt of a metal selected from among magnesium, manganese and iron. In the formulae, Ar is aryl, X is a sulfur atom, an oxygen atom, or an imino group; R1 and R2 are each a hydrogen atom or a group selected from among alkyl groups and aralkyl groups; and M is a hydrogen atom or an ion.

Kogo, Satoru (10-1 Araoi-cho 2-chome, Choshi-sh, Chiba 56, 〒2880056, JP)
向後 悟 (〒56 千葉県銚子市新生町2丁目10番地の1 ヤマサ醤油株式会社内 Chiba, 〒2880056, JP)
Osawa, Kazuomi (10-1 Araoi-cho 2-chome, Choshi-sh, Chiba 56, 〒2880056, JP)
Application Number:
Publication Date:
December 29, 2010
Filing Date:
June 22, 2010
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YAMASA Corporation (10-1, Araoi-cho 2-chome Choshi-sh, Chiba 56, 〒2880056, JP)
ヤマサ醤油株式会社 (〒56 千葉県銚子市新生町2丁目10番地の1 Chiba, 〒2880056, JP)
Kogo, Satoru (10-1 Araoi-cho 2-chome, Choshi-sh, Chiba 56, 〒2880056, JP)
向後 悟 (〒56 千葉県銚子市新生町2丁目10番地の1 ヤマサ醤油株式会社内 Chiba, 〒2880056, JP)
International Classes:
C07H19/207; A61P11/00; A61P43/00; A61K31/7076
Domestic Patent References:
Foreign References:
Other References:
QIANWEI HAN ET AL.: "One-Flask Synthesis of Dinucleoside Tetra- and Pentaphosphates", ORG. LETT., vol. 8, no. 10, 2006, pages 2075 - 2077, XP003020699, DOI: doi:10.1021/ol060491d
PENDERGAST W. ET AL.: "Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphates", BIOORG. MED. CHEM. LETT., vol. 11, no. 2, 2001, pages 157 - 160, XP004314837, DOI: doi:10.1016/S0960-894X(00)00612-0
HYOJIN KO ET AL.: "Synthesis and potency of novel uracil nucleotides and derivatives as P2Y2 and P2Y6 receptor agonists", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 16, no. 12, 2008, pages 6319 - 6332, XP022710022, DOI: doi:10.1016/j.bmc.2008.05.013
HIROAKI SAWAI ET AL.: "Mg (II) ion-mediated conversion of mono- and oligonucleotides to 5'- polyphosphates in aqueous solution", TETRAHEDRON LETTERS, vol. 34, no. 30, 1993, pages 4801 - 4804
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