WHEREIN R1 IS A HYDROGEN ATOM, A LOWER ALKOXY GROUP, ETC.; R2 IS A HYDROGEN- OR LOWER ALKYL-SUBSTITUTED PHENYL GROUP, ETC.; R3 IS A HYDROGEN ATOM OR A LOWER ALKYL GROUP, ETC; R4 IS A HYDROGEN ATOM OR A LOWER ALKYL; AND R5 IS A HYDROXY GROUP, ETC., IS OBTAINED BY REACTING A CORRESPONDING N1-ACYL PHENYLHYDRAZINE DERIVATIVE OR A MINERAL ACID SALT THEREOF WITH A CORRESPONDING PHENYL KETONE COMPOUND. THE TYPICAL EXAMPLES THEREOF ARE 1-(P-CHLOROBENZOYL)2-PHENYL 5-METHOXY - 3 - INDOLYACETICA CID AND 1-(PMETHYLBENZOYL)-2-PHENYL - 5 - METHOXY - 3 - INDOLYLACETIC ACID. THE COMPOUNDS THUS OBTAINED HAVE REMARKABLE ANTIINFLAMMATORY, ANALGESIC AND ANTIPYRETIC ACTIONS.
摘要:
A NOVEL FATTY ACID AMIDE HAVING ACTION TO LOWER CHOLESTEROL IN THE BLOOD WHICH IS COMPOSED OF AN A-ALKYLBENZYLAMINE CONTAINING IN THE A-POSITION AN ALKYL GROUP HAVING 5-17 CARBON ATOMS AND A MONOCARBOXYLIC ACID CONTAINING A SATURATED OR UNSATURATED HYDROCARBON GROUP HAVING 15-19 CARBON ATOMS. THE FATTY ACID AMIDE IS PREPARED BY REACTING SAID MONOCARBOXYLIC ACID, A REACTIVE DERIVATIVE THEREOF OR NATURAL FAT WITH SAID A-ALKYLBENZYLAMINE.
WHEREIN A, B, R1 AND R2 ARE THE SAME AS DEFINED ABOVE AND X IS HALOGEN OR HYDROXYL, AND IF NECESSARY, ESTERIFYING OR HYDROLYZING THE RESULTING CONDENSATIN PRODUCT. IN THE PRESENCE OF AN ALKALI. ALTERNATIVELY, THEY ARE PRODUCED BY REACTING THE PHENOL DERIVATIVE WITH A CARBOXYLIC ACID DERIVATIVE OF THE FORMULA,
(B-PHENYL)-O-C(-R1)(-R2)-CO-A
WHEREIN R1 AND R2 EACH IS HYDROGEN OR LOWER ALKYL, A IS HYDROXYL OR ALKOXY; AND B IS CYCLOALKENYL, 2-BENZOTHIAZOLYL OR 2-BENZOXAZOLYL. THESE COMPOUNDS ARE PREPARED BY REACTING A PHENOL DERIVATIVE OF THE FORMULA,
B-PHENOL
WITH CHLOROFORM AND A CARBONYL COMPOUND OF THE FORMULA,
R1-CO-R2 NOVEL ANTI-ATHEROSCLEROSIS AGENTS OF THE FORMULA,
NOVEL AMIDE COMPOUNDS HAVING ANTIATHEROSCLEROSIS ACTIONS WHICH ARE REPRESENTED BY THE FORMULA: WHEREIN R REPRESENTS A C15-C25, STRAIGHT, CHAIN OR BRANCHED-CHAIN, NATURAL OR SYNTHETIC SATURATED OR UNSATURATE ALIPHATIC GROUP HAVING OR NOT HAVING HYDROXYL GROUP; R1, R2, R3 AND R4 REPRESENT INDIVIDUALLY A HYDROGEN ATOM, A LOWER ALKYL GROUP, A LOWER ALKOXY GROUP OR A HALOGEN ATOM BUT CANNOT BE HYDROGEN ATOMS AT THE SAME TIME. THE ABOVE-MENTIONED AMIDE COMPOUNDS CAN BE USED AS DRUGS. THEY CAN BE USED BY ADDING THEM TO FOOD-STUFF ADDITIVES SUCH AS BUTTER AND THE LIKE FOR PREVENTING THE DEPOSITION OF CHOLESTEROL ONTO THE WALLS OF BLOOD VESSELS.