Patent ID: 6066731
Filing Date: 2000-05-23
Classification: C07D,Y02P

Abstract:
A process for the bis-aminomethylation of the unsubstituted positions on the benzene ring of .delta.-tocopherol, which process comprises forming a reaction mixture of a Mannich reagent and said .delta.-tocopherol wherein the mole ratio of said Mannich reagent to said .delta.-tocopherol in said reaction mixture is in a range from 2.5:1 to 10:1, said Mannich reagent being obtained by a process which comprises reacting formaldehyde or a formaldehyde-producing compound in the absence of a solvent with a secondary amine of the formula: ##STR7## wherein R.sup.1 and R.sup.2 are the same or different and are C.sub.1-6 -alkyl, C.sub.2-6 -hydroxyalkyl or C.sub.2-6 -alkoxyalkyl, or taken together with the nitrogen atom to which they are attached form a 5- to 8-membered heterocyclic ring, which is unsubstituted or substituted by C.sub.1-6 -alkyl, and which heterocyclic ring contains at most one additional heteroatom selected from the group consisting of oxygen and nitrogen,wherein the ratio of said formaldehyde or formaldehyde-producing compound to said secondary amine in said reaction in mole equivalents is in the range from 0.7:1 to 1.2:1, to obtain said Mannich reagent, by which process the benzene ring of said .delta.-tocopherol is bis-aminomethylated.