PURPOSE: To obtain a new α, α-dialkylbenzyl derivative useful as inhibitors for enzyme 5-LO, i.e., an inhibitor for biosynthesis of leucotriene.
CONSTITUTION: A derivative of formula I (wherein Ar1 is phenyl or naphthyl; A1 is a direct bond to X1 or is a 1-3C alkylene; X1 is oxy, thio, sulphinyl; R3 is one or two substituent(s) optionally present on phenyl selected from halogen, hydroxy and 1-4C alkyl, etc.; R1 and R2 are one or two substituent(s) selected from 1-4C alkyl, 2-4C alkenyl; R1 and R2 are each a 1-4C alkyl or 2-4C alkenyl, provided that both of R1 and R2 are not methyl or fluoromethyl; and Q is cyano or amino) and pharmaceutically acceptable salts thereof, such as 2- ethyl-2-[3-(naphth-2-ylmethoxy)phenyl]butyronitrile, is provided. The compd. of the formula I is obtained by coupling a compd. of the formula; Ar1-A1-X1-H with a compd. of formula II (wherein Z is an eliminable group) in the presence of a base in an inert solvent with use of a palladium catalyst at about 100°C.
| WO/2001/021575 | ANTI-INFLAMMATORY NITRO- AND THIA- FATTY ACIDS |
| WO/2018/159522 | FOOD COMPOSITION AND MEDICAL COMPOSITION FOR PREVENTING OR ALLEVIATING METABOLIC SYNDROME |
| WO/2007/067048 | TREATMENT OF BARRETT'S ESOPHAGUS |
DEIBUITSUDO UOOTAASON
ICI PHARMA