NEW MATERIAL: The compd. having the part of formula I (X is -O-, -NH-; (n) is 1, 2; Z is a hydrophobic anchor).
EXAMPLE: (3S)-4-[[2,4-dichloro-6-[(4-fluorophenyl) methoxy]phenyl]methoxy]methylphosphinil]-3-hydroxybutanic acid.
USE: An active inhibitor of 3-hydroxy-3-methylglutrayl-coenzyme A reductase. Effectively useful for hypocholesterolemia agents, etc., in order to suppress the biosynthesis of cholesterol.
PROCESS: The compd. of formula II is first brought into reaction with the compd. of formula III (Ra is a lower alkyl) and thereafter, the phosphinic acid of formula IV is obtd. by phosphate cleavage. The phosphinic acid is processed with oxalyl chloride in methylene chloride and is then brought into reaction with the compd. of formula V and is further processed with (C2H5)3N and a catalytic amt. of 4-dimethylaminopyridine to obtain the compd. of formula VI (Rc is Ra). Finally, the compd. is hydrolyzed after silyl ester cleavage.
| WO/2022/078416 | NOVEL GLUTAMINE ANALOGS |
| WO/1998/022480 | PHOSPHORUS CONTAINING ARYLOXY OR ARYLTHIO PROPANOLAMINE DERIVATIVES |
SUKOTSUTO ADAMUSU BIRAA
ERITSUKU MAIKERU GOODON
