METHOD OF SYNTHESIS OF PYRIMIDINE DERIVATIVE, INTERMEDIATE COMPOUNDS AND METHOD OF THEIR SYNTHESIS Russian patent published in 2001 - IPC

Abstract RU 2174978 C2

FIELD: organic chemistry, heterocyclic compounds, chemical technology. SUBSTANCE: invention relates to the improved method of synthesis of 5,6-dimethyl-2-(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydroisoquinoline-2-yl)-pyrimidine of the formula (I) , possibly, in the form of R(+)- or S(-)-isomers or salts of acid addition. Indicated compound shows an anti- -ulcer effect, inhibits gastric acid release and can be used in pharmaceutical industry. Compound of the formula (I) is synthesized by interaction of compound of the formula (IIA) with 1-methyl-1,2,3,4-tetrahydroisoquinoline of the formula (III) , possibly, in the form of R(+)- or S(-)-isomer, possibly, in the presence of solvent, for example, N,N-dimethyl-formamide, dimethylsulfoxide, n-butanol, ethylene glycol and others in the presence of the base, for example, triethylamine, N,N-dimethylaniline, pyridine, potassium acetate. Invention relates to also novel compounds of the formula (II) where R means hydroxy-group or halogen atom and to method of synthesis of compound of the formula (IIA). EFFECT: improved method of synthesis. 10 cl,, 3 dwg, 29 ex

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RU 2 174 978 C2

Authors

Khong Ju. Va

Li Jung Nam

Kim Khong Bae

Dates

2001-10-20Published

1997-04-30Filed