（２Ｒ）−２−フルオロ−２−Ｃ−メチル−Ｄ−リボノ−γ−ラクトン類前駆体の製造方法

Title:

（２Ｒ）−２−フルオロ−２−Ｃ−メチル−Ｄ−リボノ−γ−ラクトン類前駆体の製造方法

Document Type and Number:

Japanese Patent JP5716500

Kind Code:

B2

Abstract:

In the presence invention, a (2R)-2-fluoro-2-C-methyl-D-ribono-³-lactone precursor is produced in the form of a ring-opened fluorinated compound by reaction of a 1,2-diol with sulfuryl fluoride (SO 2 F 2 ) in the presence of an organic base and, optionally, a fluoride ion source. The production method of the present invention secures less number of process steps as compared to the conventional production method (shortening of three steps: cyclic sulfurous esterification, oxidation and ring-opening fluorination to one step) and satisfies the requirements for industrial production (high yield and high reproductivity). The thus-obtained (2R)-2-fluoro-2-C-methyl-D-ribono-³-lactone precursor is useful as an important intermediate for the synthesis of 2'-deoxy-2'-fluoro-2'-C-methylcytidine with antivirus activity.

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Inventors:

Akio Ishii
Nagura Yuuri
Hideyuki Tsuruta

Application Number:

JP2011082364A

Publication Date:

May 13, 2015

Filing Date:

April 04, 2011

Export Citation:

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Assignee:

Central Glass Co., Ltd.

International Classes:

C07C303/24; C07C305/10; C07D317/30

Domestic Patent References:

JP2008007488A
JP2006290870A

Foreign References:

WO2006031725A2
WO2008045419A1
WO2009075186A1
WO2009025169A1
WO2010047266A1

Other References:

WANG, P., et al, An Efficient and Diastereoselective Synthesis of PSI-6130: A Clinically Efficacious Inhibitor of HC,The Journal of Organic Chemistry,2009年,vol.74, No.17,6819-6824
L'HEUREUX, A., et al,Aminodifluorosulfinium Salts: Selective Fluorination Reagents with Enhanced Thermal Stability and Ea,The Journal of Organic Chemistry,2010年,vol.75, No.10,3401-3411

Attorney, Agent or Firm:

Makoto Koide

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