NOVEL PRODUCTION PROCESS FOR MACROLIDE COMPOUND

WIPO Patent Application WO/2007/142187

A1

The invention has been achieved as a result of intensive studies of a production process such that a macrolide compound (II) useful as a pharmaceutical can be produced efficiently at a high yield and a low cost and can be stably supplied. The inventors found that the above object is achieved by using a macrolide compound (I) (for example, tacrolimus) as a raw material, and performing Wacker oxidation with the use of a dialkyl sulfoxide, an alkyl aryl sulfoxide or a diaryl sulfoxide as a solvent, or with the use of a palladium complex containing a dialkyl sulfoxide, an alkyl aryl sulfoxide or a diaryl sulfoxide as a ligand. According to theproduction process of this application, it becomes possible to stably supply the macrolide compound (II) from the expensive raw material (I) such as tacrolimus efficiently at a high yield. Thus, it is an industrially very useful process and can provide the macrolide compound (II) which is very useful as a pharmaceutical.

KUBOTA ARIYOSHI (JP)
OKAWA KAZUO (JP)
WATANABE MASARU (JP)
IKE KAZUO (JP)

PCT/JP2007/061286

December 13, 2007

June 04, 2007

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ASTELLAS PHARMA INC (JP)
KUBOTA ARIYOSHI (JP)
OKAWA KAZUO (JP)
WATANABE MASARU (JP)
IKE KAZUO (JP)

C07D498/18; C07B61/00

JPH02502463A	1990-08-09
JPH05500215A	1993-01-21
JP2004137192A	2004-05-13
JP2004161963A	2004-06-10
JPH07500613A	1995-01-19
JPH0827055A	1996-01-30

CLIVE D.L.J. ET AL.: "New Low-Valent Titanium Reagents for Dicarbonyl Coupling and Their Use in a General Method of Annulation", J. ORG. CHEM., vol. 56, no. 22, 1991, pages 6447 - 6458, XP003020192

MORITA, Hiroshi et al. (3-11 Nihonbashi-Honcho 2-chom, Chuo-ku Tokyo 11, JP)

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