| 摘要 |
<p>PURPOSE: To obtain a new 2-amino-3-phenylpropionic acid derivative high in safety, having a hypoglycemic action and a blood lipid-reducing action, and useful for therapeutic medicines for diabetes, hyperlipidemia, etc. CONSTITUTION: The derivative (salt) of formula I [R1 is OH, a lower alkoxy, phenoxy, amino, etc.; R2 , R3 are H, a lower alkyl, a five or six-membered aromatic heterogeneous ring group-substituted lower alkyl, etc.; R4 is H, nitro, a lower alkoxy, etc., W is O, carbonyl; m is 0-2; A is a group of formula II (X is O, N, S; R5 , R6 are H, a lower alkyl, phenyl, etc.), etc.], e.g. (S)-2-t- butoxycarbonylamino-3- 4-[4-[2-(5-methyl-2-phenyl-4-oxazolyl) ethoxy]phenyl}propionic acid ethyl ester. The derivative (R1 is OH; R2 -R4 are H) is obtained e.g. by reacting a tyrosine derivative of formula III (T is H, OH; R8 is an amino-protecting group; R9 is a lower alkoxy) with an alkylating reagent, treating the obtained derivative of formula IV with an acid to release the amino-protecting group R3 , and subsequently hydrolyzing the product.</p> |
