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Title:
NOVEL PROTECTING GROUP FOR SYNTHESIZING RNA AND DERIVATIVE THEREOF
Document Type and Number:
WIPO Patent Application WO/2011/034072
Kind Code:
A1
Abstract:
A protecting group represented by general formula (I) which is stable under reaction conditions of the nucleic acid synthesis cycle, has small steric hindrance and can be removed under mild conditions using a fluoride ion as a base. In general formula (I), the oxygen atom marked by * represents the oxygen atom in a hydroxyl group at the 2'-position of a ribonucleoside, a ribonucleotide or a derivative of the same; R1 and R2 are both hydrogen atoms, or represent a halogen atom, a C1-6 alkyl group or a C1-6 haloalkyl group; R3 and R4 represent a hydrogen atom, a halogen atom, a C1-6 alkyl group or a C1-6 haloalkyl group; and R5 and R6 represent a halogen atom, a C1-6 haloalkyl group, a cyano group, a nitro group, etc.

Inventors:
WADA Takeshi (4-11-42-301, Asahi-cho Kashiwa-sh, Chiba 52, 〒2770852, JP)
和田 猛 (〒52 千葉県柏市旭町4-11-42-301 Chiba, 〒2770852, JP)
Application Number:
JP2010/065900
Publication Date:
March 24, 2011
Filing Date:
September 15, 2010
Export Citation:
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Assignee:
CHIRALGEN, LTD. (2438, Miyanoura-cho Kagoshima-sh, Kagoshima 34, 〒8911934, JP)
株式会社キラルジェン (〒34 鹿児島県鹿児島市宮之浦町2438番地 Kagoshima, 〒8911934, JP)
WADA Takeshi (4-11-42-301, Asahi-cho Kashiwa-sh, Chiba 52, 〒2770852, JP)
International Classes:
C07H19/067; C07F7/18; C07F9/6558; C07F9/6561; C07F9/6584; C07H19/10; C07H19/167; C07H19/20; C07H21/02; C07C43/13
Domestic Patent References:
WO2005023828A1
WO2005092909A1
WO2006022323A1
WO2005023828A1
WO2006022323A1
Other References:
See also references of EP 2479182A4
J. AM. CHEM. SOC., vol. 109, 1987, pages 7845
HELVETICA CHIMICA ACTA, vol. 81, 1998, pages 1545
TETRAHEDRON LETT., vol. 45, 2004, pages 9529
HELVETICA CHIMICAACTA, vol. 81, 1998, pages 1545
CHEM. REV., vol. 80, 1980, pages 429
GREEN ET AL.: "Protective Groups in Organic Synthesis", 1999, JOHN WILEY & SONS, INC.
JOURNAL OF FLUORINE CHEMISTRY, vol. 24, 1984, pages 531 - 533
Attorney, Agent or Firm:
SIKs & Co. (8th Floor, Kyobashi-Nisshoku Bldg. 8-7, Kyobashi 1-chome, Chuo-k, Tokyo 31, 〒1040031, JP)
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