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NEW 2-AROMATIC RING-SUBSTITUTED-3-PHENYLPROPIONIC ACID OR ACRYLIC ACID DERIVATIVE

机译:新的2-芳环取代3-苯丙酸或丙烯酸衍生物

摘要

PURPOSE: To obtain the new derivative strong in a hypoglycemic action and a blood lipid-reducing action, and extremely little in toxicity. ;CONSTITUTION: The derivative (salt) of formula I [R1 is OH, a lower alkoxy, phenyl, amino, etc.; R2 is a five or six-membered aromatic heterogeneous single ring group, a substituted phenyl; W is O, carbonyl; m is 0-2; A is a group of formula II (X is O, N, S; R6, R7 are H, a lower alkyl, phenyl, etc.), etc.], e.g. 3-{4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl}-2-(2-pyridyl)acrylic acid ethyl ester. The derivative is obtained by reacting a (4-hydroxy)benzaldehyde of formula III (T is H, OH) with an acetic acid derivative of formula: R2-CH2- COR1, reacting the obtained phenylacrylic acid derivative of formula IV with an alkylating agent of formula: A-(CH2)mR9 (R9 is OH, a halogen, p- toluenesulfonyloxy, etc.), and subsequently reducing the obtained phenylacrylic acid derivative of formula V.;COPYRIGHT: (C)1996,JPO
机译:目的:获得具有强降血糖作用和降血脂作用且毒性极低的新衍生物。 ;组成:式I [R 1 的衍生物(盐)为OH,低级烷氧基,苯基,氨基等; R 2 是五元或六元芳族杂单环,是取代的苯基; W是O,羰基; m为0-2; A是一组式II的基团(X是O,N,S; R 6 ,R 7 是H,低级烷基,苯基等)等。 ],例如3- {4- [2-(5-甲基-2-苯基-4-恶唑基)乙氧基]苯基} -2-(2-吡啶基)丙烯酸乙酯。通过使式III(T为H,OH)的(4-羟基)苯甲醛与式R 2 -CH 2 的乙酸衍生物反应获得该衍生物-COR 1 ,使获得的式IV的苯基丙烯酸衍生物与式A-(CH 2 m R < Sub> 9 (R 9 是OH,卤素,对甲苯磺酰氧基等),随后还原得到的式V的苯基丙烯酸衍生物。版权所有:(C)1996 ,日本特许厅

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