To obtain the subject compound in a high yield by the reaction of an alkyne with a carbonyl compound and an amine in the presence of a heterogeneous catalyst.
This compound, a hydroxyalkyl-substituted aminoalkyne of formula IV [e.g. 3-(di-2-hydroxyethylamino)propyne], is obtained by reaction of an alkyne of formula I (R1 is H, an alkyl, hydroxyalkyl, etc.) with a carbonyl compound of formula II (R2 and R3 are each H, an alkyl, aryl, alkoxy, etc..) and an amine of formula III (R4 and R5 are each H, an alkyl, hydroxyalkyl, etc., or joined together with a bound N atom to form a five- or six-membered ring) in the presence of a heterogeneous catalyst such as an acetylated copper catalyst carried on a bismuth-doped silicate support. By virtue of this method, the objective desired aminoalkyne can be obtained in high yield without the need of any special means for pH adjustment.
PREISS THOMAS DR
HENKELMANN JOCHEM DR
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