Field
     Production method, medical drug, cancer treatment

Keywords
     Antiestrogen effect, hormone-dependent breast cancer drug, tamoxifen derivative,
     osteoporosis prophylaxis, three-component coupling reaction,
     double bond rearrangement reaction

Advantages
     According to this invention, it becomes possible to manufacture DOROROKISHIFEN useful
     as an anticancer agent at the very short process of only 4 processes, it can mass-produce
     DOROROKISHIFEN inexpensive by this, and is very significant in the field of drugs manufacture
     and a cancer therapy.

Abstract
To provide a new droloxifene production method for efficiently producing droxifene with decreased reaction steps.
Droloxifene is produced by successively carrying out a three-component coupling reaction using a 3-alkanoyloxybenzaldehyde, a trimethylcinnamylsilane and a 2-haloethoxybenzene as starting compounds, a reaction for eliminating an acyloxy group and forming a dimethylamino group, and a double bond rearrangement reaction as reaction steps.


Inventor
     Prof. Isamu Shiina et al.　(Tokyo University of Science)


Patent Publication No
     (APPLICATION NUMBER, FILING DATE)
     JP2010-134878 (Jun. 14, 2010, divisional application）
     (PUBLICATION NUMBER, PUBLICATION DATE)
     JP2010-195832 (Sep. 9, 2010） 

Publication
     Bioorganic & Medicinal Cem.15(2007)7599-7617
     Bioorganic & Medicinal Chem. Letter 17(2007)2421-2424
     Biochemical Pharmacology 75(2008)1014-1026
     Cancer Sci. March 2008,99, 608-614


Internal file number
     LSP:100
     T2010-020 (T2004-103 )

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