摘要:
This invention relates to chlorinated derivatives of 1-(2- Delta 2-imidazolinyl)-2,2-diarylcyclopropanes and their acid addition salts as new industrial products, to the process for their preparation and to their therapeutic application such as antiinflammatory and anti-arrhythmic agents.
摘要:
The invention relates to compounds of the formula
IN WHICH R represents the hydrogen atom, the fluorine atom, the bromine atom, a lower C1-C5 alkyl group, a lower C1-C5 alkoxy group, and R1 represents the hydrogen atom, a lower C1-C5-alkyl group, an alkynyl group with at most 5 carbon atoms; an alkenyl group with at most 5 carbon atoms, a lower C1-C5 hydroxy alkyl group or an aralkyl group whose aromatic radical is capable of substitution, and to their acid addition salts as new industrial products. These compounds and their non-toxic acid addition salts can be used for therapeutic purposes such as in the treatment of cardiovascular disorders.
摘要翻译:本发明涉及下式化合物:其中R代表氢原子,氟原子,溴原子,低级C1-C5烷基,低级C1-C5烷氧基,R1代表氢原子,低级C1 C 5 - 烷基,最多5个碳原子的炔基; 具有至多5个碳原子的烯基,较低的C 1 -C 5羟基烷基或芳基能够被取代的芳烷基,以及作为新的工业产品的它们的酸加成盐。
AND THE ACID ADDITION SALTS OF SAID BASES WITH PHARMACEUTICALLY ACCEPTABLE ACIDS, WHEREIN R REPRESENTS HYDROXY OR LOWER ALKOXY, R1 REPRESENTS PHENYL OR PHENYL MONOSUBSTITUTED WITH HALO, LOWER ALKYL, LOWER ALKOXY OR TRIFLUOROMETHYL, R2 AND R5, ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY, LOWER ALKYL, LOWER ALKOXY, HALO (LOWER) ALKYL AND HALOGEN, AND R3 AND R4 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALKYL.
摘要:
NEW FLUORO DERIVATIVES OF ARALKYLAMINE COMPOUNDS, PARTICULARLY 2-(2-PHENYL-1,1,2,2-TETRAFLUOROETHYL) BENZYLAMINE AS WELL AS THE N-ALKYL AND THE N,N-DISLKYL DERIVATIVES THEROF ARE PREPARED BY REACTION OF 2-BROMOBENZONITRILE WITH BENZYLMAGNESIUM CHLORIDE TO PRODUCE 2''-BROMO-2PHENYLACETOPHENONE; OXIDATION OF SAID ACETOPHENONE WITH SELENOUS ACID TO PRODUCE 2-BROMOBENZIL; CONVERSION OF THE BENZIL COMPOUND BY TREATMENT WITH SULFUR TETRAFLUORIDE TO THE CORRESPONDING 2-BROMO-A,A,A'',A2-TETRAFLUOROBENZYL; FOLLOWED BY REACTION OF THE 2-BROMOBIBENZYL COMPOUND WITH A METAL CYANIDE TO PRODUCE THE CORRESPONDING 2-(2-PHENYL1,1,2,2-TETRAFLUOROETHYL) BENZONITRILE. THIS NITRILE COMPOUND IN THEN CORRESPONDING BENZYLAMINE, WHICH IS THEN PRODUCE THE CORRESPONDING BENZYLAMINE, WHICH IS THEN CONVERTED, IF DESIRED, TO THE N-ALKYL AND/OR N,N-DIALKYL 2-(2-PHENYL-1,1,2,2-TETRAFLUOROETHYL) BENZYLAMINE. ALTERNATIVELY, THE NITRILE OR THE PRECURSOR BROMOBIBENZYL CAN BE CONVERTED BY GRINARD REACTIONS TO THE CORRESPONDING A-ALKYL OR A,A-DIALKYLBENZYLAMINE WHICH CAN THEN BE CONVERTED IF DESIRED TO THE CORRESPONDING N-ALKYL AND/OR N,NDIALKYL SUBSTITUTED BENZYLAMINE COMPOUND. THE PHENYLTETRAFLUOROETHYLBENZYLMINE AS WELL AS ITS N-ALKYL AND N, N-DIALKYL DERIVATIVES ARE ACTIVE AS ANTIARRHYTHMIC AGENTS.
WHERE R IS ISOPROPYL, PHENYL OR HYDROXYETHYL AND R1 IS HYDROGEN OR CHLORINE. THE COMPOUNDS HAVE UTILITY AS TRANQUILIZING AGENTS FOR WARN-BLOODED ANIMALS.