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
展开▼
机译：技术领域本发明涉及一种获得通式的1'-芳基六氢-1H-螺环[嘧啶-5,2'-吡咯嗪] -2,4,6（1H，3H，5H）-三聚体的方法我可以用作镇静剂，抗惊厥药和胆汁溶解药。在通式I（am）中<图像文件=“ 00000008.JPG” he =“ 27” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 34” />，Ar = C 6 H 5 ，R = H（Ia）; Ar = 4-CH 3 OC 6 H 4 ，R = H（Ib）; Ar = 4-（CH 3 ） 2 NC 6 H 4 ，R = H（Ic）; Ar = C 6 H 5 ，R = 3-C 6 H 5 OC 6 H 4 （Id）; Ar = 4-CH 3 OC 6 H 4 ，R = 3-C 6 H 5 OC 6 H 4 （即）; Ar = 4-（CH 3 ） 2 NC 6 H 4 ，R = 3-C 6 H 5 OC 6 H 4 （Ig）; Ar = C 6 H 5 ，R = 2,4-Cl 2 C 6 H 3 （Ih）; Ar = 4-CH 3 OC 6 H 4 R = 2,4-Cl 2 C 6 H 3 （II）; Ar = 4-（CH 3 ） 2 NC 6 H 4 ，R = 2,4-Cl < Sub> 2 C 6 H 3 （Ij）; Ar = C 6 H 5 ，R = 3,4-（CH 3 O） 2 C 6 H 3 （Ik）; Ar = 4-CH 3 OC 6 H 4 ，R = 3,4-（CH 3 O） 2 C 6 H 3 （II）; Ar = 4-（CH 3 ） 2 NC 6 H 4 ，R = 3,4-（CH 3 O） 2 C 6 H 3 （Im）。获得Ia-m化合物的方法包括通过加热等摩尔量的相应的5-（芳基亚甲基）-2,4,6-嘧啶-2,4,6（1H，3H，5H）-三酮进行三组分杂环化公式II（ac）的<图像文件=“ 00000009.JPG” he =“ 25” imgContent =“ undefined” imgFormat =“ JPEG” wi =“ 38” />，其中Ar = C 6 H 5 （IIa）; Ar = 4-CH 3 OC 6 H 4 （IIb）; Ar = 4-（CH 3 ） 2 NC 6 H 4 （IIb）; L-脯氨酸（III）和相应的通式IV（a-d）的醛RCHO，其中R ＝ H（IVa）; R = 3-C 6 H 5 OC 6 H 4 （IVb）; R = 2,4-Cl 2 C 6 H 3 （IVc）; R = 3,4-（CH 3 O） 2 C 6 H 3 （IVd）。杂环化反应最好在干燥的甲苯中进行17小时。效果：提高收率; 2 cl，16 ex
展开▼
