| abstract |
NEW MATERIAL: A compound of formula I {Q is a 1-5C alkyl, 6-10C aryl, 7-15C aralkyl, etc.; R 3 and R 5 are each H, a 1-5C hydroxyalkyl, a 1-5C alkyl, etc.; R 4 is CHR 0 R; R 0 is H, a 1-5C alkyl, etc.; R is O-(CO) p2 -(A) p1 R 1 , etc., [p1 and p2 are each 0 or 1, provided that they are not both 0; R 1 is H, an aryl, etc.; A is formula II, etc., (R 2 is H, a 1-5C alkoxy, etc.)]}. n EXAMPLE: (±)-Cis-3-Ethyl-4-hydroxymethyl-2-azetidinone. n USE: Anti-hypercholesterolemia agents useful for arteriosclerosis, hyperlipidemia, etc. n PROCESS: Trimethylsilylamine of formula III is added to an α,β-unsaturated aldehyde to give a β-lactam of formula IV. The product is converted into the alcohol, and the hydroxy group of the alcohol is protected, sulfonylated, deprotected and acylated to give a compound of formula I. n COPYRIGHT: (C)1991,JPO |