ES317241A1 - A procedure for the preparation of gammapicolyl derivatives. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

A process for the preparation of gamma-picolyl derivatives, which consists in reacting a 4-picolyl-metal compound of the general formula III ** (See formula) ** where the symbol M represents sodium, potassium, lithium or a halogen metal, with a ketone of the general formula IV ** (See formula) ** wherein R1 and R2 each represent, independently, lower alkyl, halogen-lower alkyl, lower alkenyl, lower alkynyl, aralkyl, aralkenyl, lower aliphatic alkylenic ether, lower alkylenic ether, lower alkyl aralkyl ether, a 5- or 6-membered heterocyclic group, a bicyclic heterocyclic group with 7 to 10 atoms in the heterocyclic nucleus, a cycloalkyl group of 3 to 8 carbon atoms, amino, substituted amino, aminomethyl, aminomethyl monosubstituted by lower alkyl and unsubstituted by alkyl lower, unsubstituted aminomethyl wherein the two substituents, together, represent lower alkylene, lower aza-alkylene, lower oxa-alkylene and lower thia-alkylene, such that the unsubstituted amino group is part of a 5-6 membered heterocyclic nucleus, unsubstituted phenyl or phenyl bearing, at least one of the following substituents: amino, substituted amino, hydroxy, hal Oxygen, trifluoromethyl, lower alkyl and lower alkoxy, with the proviso that when both R 1 and R 2 represent such a substituted phenyl or phenyl group, at least one of the symbols R 1 and R 2 is a substituted phenyl such as hereinabove. define; and where R1 and R2, taken collectively with the carbon atom to which they are attached, represent a cycloalkyl group of 3 to 8 carbon atoms, an unsubstituted monocyclic heterocyclic group and substituted by lower alkyl, of 5 to 8 carbon atoms, which it contains at least one heteroatom of nitrogen, sulfur and/or oxygen, a bicyclic heterocyclic group of 5 to 10 carbon atoms, containing at least one heteroatom of nitrogen, sulfur and/or oxygen, a 9-substituted xanthene, an -substituted-5H-dibenzo [a, d] cycloheptene and a 5-substituted-10,11-dihydro-5H-dibenzo [a, d] cycloheptene, in dehydrating, if desired, an alcohol obtained, in hydrogenating, if desired, the double bond thus created, in the presence of a catalyst, and in transforming, if desired, the above reaction products into an acid addition salt . (Machine-translation by Google Translate, not legally binding)