METHOD FOR OBTAINING 1'-ARYLHEXAGYRO-1N-SPIRO[PYRIMIDINE-5,2'-PYRROLYSINE]-2,4,6(1H, 3H, 5H)-TRIONES Russian patent published in 2018 - IPC C07D487/10 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of obtaining 1'-arylhexahydro-1H-spiro [pyrimidine-5,2'-pyrrolizine]-2,4,6(1H,3H,5H)-trimones of general formula I which can be used as sedatives, anticonvulsant and cholinolytic agents. In the general formula I (a-m) , Ar=C₆H₅, R=H (Ia); Ar=4-CH₃OC₆H₄, R=H (Ib); Ar=4-(CH₃)₂NC₆H₄, R=H (Ic); Ar=C₆H₅, R=3-C₆H₅OC₆H₄ (Id); Ar=4-CH₃OC₆H₄, R=3-C₆H₅OC₆H₄ (Ie); Ar=4-(CH₃)₂NC₆H₄, R=3-C₆H₅OC₆H₄ (Ig); Ar=C₆H₅, R=2,4-Cl₂C₆H₃ (Ih); Ar=4-CH₃OC₆H₄ R=2,4-Cl₂C₆H₃ (Ii); Ar=4-(CH₃)₂NC₆H₄, R=2,4-Cl₂C₆H₃ (Ij); Ar=C₆H₅, R=3,4-(CH₃O)₂C₆H₃ (Ik); Ar=4-CH₃OC₆H₄, R=3,4-(CH₃O)₂C₆H₃ (Il); Ar=4-(CH₃)₂NC₆H₄, R=3,4-(CH₃O)₂C₆H₃ (Im). The method for obtaining compounds of Ia-m consists of three-component heterocyclization by heating equimolar amounts of the corresponding 5-(arylmethylidene)-2,4,6-pyrimidine-2,4,6(1H,3H,5H)-trione of general formula II (a-c) , where Ar=C₆H₅ (IIa); Ar=4-CH₃OC₆H₄ (IIb); Ar=4-(CH₃)₂NC₆H₄ (IIb); L-proline (III) and the corresponding aldehyde of general formula IV (a-d) RCHO, where R=H (IVa); R=3-C₆H₅OC₆H₄ (IVb); R=2,4-Cl₂C₆H₃ (IVc); R=3,4-(CH₃O)₂C₆H₃ (IVd). Preferably the heterocyclization is carried out for 17 hours in dried toluene.

EFFECT: increasing the yield.

2 cl, 16 ex