NOVEL PYRIMIDINE THIONE COMPOUND AND PROCESS FOR ITS PREPARATION

摘要

Compound IV was obtained by the halogenation of dihydroxycycloalkapyrimidine(V) with halogenating agent, followed by the reaction with ammonia water in the presence of solvents to give III. Compound II(X= halogen atom or sulfate acid residue) was obtained by introduction of R in III, followed by the substitution reaction of alkali metal hydrosulfide(M-SH; M= lithium, sodium or potassium) to give 4-amino-3-substituted-cycloalkapyrimidine-2-thione derivatives(I; R= amino group, C1-4 alkyl or C3-7 cycloalkyl group, n= 2- 7). Thus, 10 g mesitylene sulfonyl hydroxylamine in 20 ml dichloromethane was dropped in 5 g of 2-chloro-6,7-dihydro-5H-cyclopentapyrimidin-4-yl amine in 100 ml dichloromethane, followed by addition of 2.5 g sodium hydrosulfide for 30 minutes to give 3 g 3,4-diamino-3,5,6,7-tetrahydrocyclopentapyrimidine-2-thione.