반응 #967323

반응 방정식

sodium [1-methyl-4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate

3-cyclopropylaniline

CH2Cl2 MeOH

N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride

→

N-(3-cyclopropylphenyl)-2-[1-methyl-4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide

수율 48.2%

용매

pyridine

N,N-dimethylformamide

반응 조건

후처리

1. 1
   기타The product is prepared
2. 2
   추출After extractions
3. 3
   기타with ethyl acetate and silica column purification of the residue
4. 4
   기타obtained

실험 절차

The product is prepared according to the procedure described in example 5, using 200 mg of sodium [1-methyl-4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetate prepared in stage 1 of example 68, 194 mg of 3-cyclopropylaniline (prepared according to Wallace et al. in Tetrahedron Lett. 2002, 43, 6987), and 185 mg of N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride in a mixture of 0.12 ml of pyridine and 4 ml of N,N-dimethylformamide. After extractions with ethyl acetate and silica column purification of the residue obtained, eluent: 95/05 CH2Cl2/MeOH, 129 mg of N-(3-cyclopropylphenyl)-2-[1-methyl-4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide are obtained in the form of a white solid, the characteristics of which are the following:

출처