Title:
SYNTHESIS METHOD OF ENTECAVIR, AND INTERMEDIATE COMPOUND THEREOF
Document Type and Number:
Japanese Patent JP2016196499
Kind Code:
A
Abstract:
PROBLEM TO BE SOLVED: To solve the problem that, though a preparation method of an intermediate 4 in a process for preparing a compound expressed in formula 1 is disclosed in international public 2004/052310A2, yield is low, and application of the method to industrial production is difficult.SOLUTION: There is provided a preparation method of a compound 4 expressed in formula 4. The method includes steps for (a) obtaining directly a cyclopentane intermediate 3 by subjecting a compound 2 to ring opening, and (b) obtaining a compound 4 by subjecting a compound expressed in formula 3 to alcoholysis or hydrolysis.SELECTED DRAWING: None
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Inventors:
ZHENG ZHIGUO
Application Number:
JP2016144062A
Publication Date:
November 24, 2016
Filing Date:
July 22, 2016
Export Citation:
Assignee:
ZHEJIANG AUSUN PHARMACEUTICAL CO LTD
International Classes:
C07F7/18; C07D309/12; C07D319/08
Domestic Patent References:
| JP2006509800A | 2006-03-23 | |||
| JPH06502390A | 1994-03-17 | |||
| JPS6468367A | 1989-03-14 | |||
| JPS6042348A | 1985-03-06 | |||
| JPS60166644A | 1985-08-29 |
Foreign References:
| WO2010074534A2 | 2010-07-01 | |||
| WO2011102806A1 | 2011-08-25 | |||
| WO2011046303A2 | 2011-04-21 | |||
| WO2011150512A1 | 2011-12-08 | |||
| WO2011150513A1 | 2011-12-08 |
Other References:
ZIEGLER, FREDERICK E. ET AL.: "Radical cyclization studies directed toward the synthesis of BMS-200475 'entecavir': the carbocyclic", TETRAHEDRON, vol. 59(45), JPN6015015203, 2003, pages 9013 - 9018, ISSN: 0003510190
THEODORA W. GREENE ET AL., PROTECTING GROUPS IN ORGANIC SYNTHESIS, vol. Third Edition, JPN7015001037, 1999, US, ISSN: 0003510191
GREENE, T. W. ET AL., PROTECTIVE GROUPS IN ORGANIC SYNTHESIS, JPN7018002439, 1991, pages 132 - 133, ISSN: 0003841119
THEODORA W. GREENE ET AL., PROTECTING GROUPS IN ORGANIC SYNTHESIS, vol. Third Edition, JPN7015001037, 1999, US, ISSN: 0003510191
GREENE, T. W. ET AL., PROTECTIVE GROUPS IN ORGANIC SYNTHESIS, JPN7018002439, 1991, pages 132 - 133, ISSN: 0003841119
Attorney, Agent or Firm:
Atsushi Aoki
Takashi Ishida
Fukumoto product
Tetsuji Koga
Yoichi Watanabe
Masaru Nakajima
Ryotaro Takei
Takashi Ishida
Fukumoto product
Tetsuji Koga
Yoichi Watanabe
Masaru Nakajima
Ryotaro Takei
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