Process for the reductive amination of aldehydes and ketones via the formation of macrocyclic polyimine intermediates
A technology for amine compounds and products is applied in the field of reductive amination of aldehydes and ketones by forming macrocyclic polyimine intermediates, which can solve the problems of polluted reactors, difficult and expensive purification of crude products, and achieves high selectivity.
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Embodiment 1
[0063] A mixture of 1,3- and 1,4-cyclohexanedicarbaldehyde (3.08 g, 22 mmol) and 1,3- and 1,4-bis(aminomethyl)cyclohexane (4.26 g, 30 mmol) were dissolved in 11g methanol. Diglyme (2.38 g) was added as an internal standard for gas chromatographic analysis. The mixture was stirred at room temperature for 30 minutes. During this time, the reactants formed an intermediate product mixture containing a majority of macrocyclic polyimine species with a molecular weight of about 490 to 1480.
[0064] A powdered nickel catalyst (Ni-5256W from Engelhard) (0.75 g) was placed in a 160 mL Parr reactor with 30 g of methanol. The reactor was purged three times with 100 psi (689 kPa) nitrogen, charged with 1000 psi (6895 kPa) hydrogen and heated to 200°C for two hours to activate the catalyst. The reactor is then cooled and the hydrogen is pumped off. The intermediate product mixture obtained above was then transferred to a reactor. Anhydrous ammonia (37.7 g, 2.22 mol) was added with sti...
Embodiment 2
[0066] Example 1 was repeated without adding diglyme. After the reductive amination was complete, the catalyst was filtered from the reaction mixture and washed twice with methanol (50 g). Combine the wash solution with the reaction mixture. Methanol was then evaporated off followed by flash evaporation at 70-75 °C / 1 mm Hg in vacuo to produce 6.61 g of 1,3- and 1,4-bis(aminomethyl)cyclohexane (91% yield alone ).
Embodiment 3
[0068] Example 1 was repeated, however the temperature in the hydrogenation step was only 120°C, the reaction time was 3 hours, and the ratio of ammonia to aldehyde groups provided by the 1,3- and 1,4-cyclohexanedicarbaldehyde starting materials 25. The yield of 1,3- and 1,4-bis(aminomethyl)cyclohexane was 88%. About 9% of 3-azabicyclo[3.3.1]nonane was formed. The presence of 3-azabicyclo[3.3.1]nonane indicates that the amination / reduction reaction did not proceed to completion within the time given, at a temperature of 120°C and with the amount of aqueous ammonia used.
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