BENZYLOXY-SUBSTITUTED PHENYLGLYCINOLAMIDE

PROBLEM TO BE SOLVED: To obtain a new compound useful for the suppression of atherosclerosis and coronary heart diseases and capable of being utilized as an antiatheroselerotic medicine. SOLUTION: A benzyloxy-substituted penylglycinolamide of formula I (A is a four to eight-membered carbon ring, etc...

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Hauptverfasser: DENZER DIRK DR, GRUETZMANN RUDI DR, BISCHOFF HILMAR DR, CONNELL RICHARD DR, BEUCK MARTIN DR, MUELLER ULRICH DR, GOLDMANN SIEGFRIED DR
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Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To obtain a new compound useful for the suppression of atherosclerosis and coronary heart diseases and capable of being utilized as an antiatheroselerotic medicine. SOLUTION: A benzyloxy-substituted penylglycinolamide of formula I (A is a four to eight-membered carbon ring, etc.; X is a single bond or a group of formula II; D and E are each H, a 3-8C cycloalkyl, etc.; R is a 3-8C cycloalky, etc.; R is H, a 4C alkyl, etc.; R is H, CH2 OH; R is hydroxy, a halogen, etc.) and its salt. The compound of formula I is obtained by activating the functional carboxyl group of a carboxylic acid of formula III and subsequently reacting the activated compound with a compound of formula IV in the presence of a base and/or an auxiliary agent in an inactive solvent (e.g. an ether compound) at a reaction temperature of 0-150 deg.C generally in the atmospheric pressure in a protecting gas atmosphere. The base used herein is usually an inorganic or organic base, and is used in an amount of 0.6-5 moles per mole of the compound of formula III.