Method for producing (R)-3-[4-(trifluoromethyl)...

Details Method for producing (R)-3-[4-(trifluoromethyl)... Method for producing (R)-3-[4-(trifluoromethyl)...

2007-05-29

2007-05-29

Saeed, Kamal A. (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C564S194000

Reexamination Certificate

active

10801141

ABSTRACT:
The present invention provides a method for easily producing an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative useful for an intermediate for pharmaceutical products, particularly an inhibitor of a cholesteryl ester transfer protein (CETP) from easily available raw materials. In the present invention, (S)-N-[4-(trifluoromethyl)phenyl]-3-hydroxypentanoic acid amide prepared from easily available raw materials leads a production of (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone to give (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide. Furthermore, (R)-4-ethyl-1-[4-(trifluoromethyl)phenyl]-2-azetidinone is reacted with a carbamic acid ester to give an (R)-3-[4-(trifluoromethyl)phenylamino]-pentanoic acid amide derivative.

REFERENCES:
patent: 3773620 (1973-11-01), Kimura et al.
patent: 5227538 (1993-07-01), Buchwald et al.
patent: 6706881 (2004-03-01), Damon et al.
patent: WO 02/088069 (2002-11-01), None
patent: WO 02/088085 (2002-11-01), None
patent: WO 02088085 (2002-11-01), None

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