It is said “Shiina method” that make possible to allylate and alkylate of aromatic aldehyde sucsessively.

Field
Synthesis Approach, Production, Medicine, Biotechnology
Keywords
Lasofoxifene, Production, Osteoporosis After Menopause, Serum Cholesterol, Cardiovascular


Abstracts
Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.

Advantages
According to this invention, as a selective estrogen receptor modulator (SERM; selective estrogen receptor modulator), It makes it possible to provide supply with RASOFOKISHIFEN or the other analogs which are especially expected as remedies, such as postmenopausal osteoporosis, cheaply and in large quantities.


Inventor
Prof. Isamu Shiina, Yoshiyuki Sano et al.
(Tokyo University of science)


Patent Publication No
(APPLICATION NUMBER, FILING DATE)
WO200751186 (Jan.25, 2007), EP20070707418 (Jan.25, 2007), US12/162068  (Jan.25, 2007)
(PUBLICATION NUMBER, PUBLICATION DATE)
WO2007086471 (A1) (Aug.2, 2007), EP1982981 (A1) (Oct. 22, 2008), US2009-0012314-A1 (Jan. 8, 2009)
(PRIORITY APPLICATION NUMBER, PRIORITY DATE)
①JP2006-0018079 (Jan.26, 2006) ②JP2007-0001114 (Jan.9, 2007)


Internal file number
G2006-008 (T2005-098, T2006-099)

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