PROCESS FOR THE PREPARATION OF SUBSTITUTED DERIVATIVES OF TETRAHYDROPYRIMIDINE AND IMIDAZOLINE

摘要

(1) Tetrahydropyrimidine and imidazoline derivs. of formula (I) and their acid-addn. salts are new. X = O or S; R1 = H or 1-3C alkyl; R2 = H, 1-6C alkyl, CHR16-(2-6C)alkenyl, (CR16R16)mR15 or CHR16-CH=CHPh; R15 = OH or Ph; R16 = H, Me or Et; m = 2,3 or 4 or when R15 = Ph, also 1; R4-R9 = H or any 1 or 2 are 1-3C alkyl; n = 0 or 1; R10 = H, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, 1-4C alkylsulphinyl, halogen or CF3; R11 = H, 1-3C alkyl or halogen; R12 = H, Me or Et. Provided that (a) when R10 = H 4-Br or 4-Me, R11 = R12 = H, X = O and n = 0, then at least 1 or R1, R2, R4, R5, R8 and R9 is other than H; (b) when R10 = R11 = R12 = H or R10 = 3-Cl, R11 = 4-Cl, R12 = H, X = O and n = 1, then at least 1 or R1, R2, R4-R9 is other than H; (c) when R10 = H or 4-Cl, R11 = R12 = H, R2 = Me and X = O, then at least 1 or R1, R4, R5, R8 and R9 and when n = 1, R6 and R7 is other than H; and (d) when R10 = H, 4-MeO or 4-Me, R11 = R12 = H, R2 = Me, X = S and n = 1, then at least 1 of R1 and R4-R9 is other than H. (2) The use as pharmaceuticals of (I) as defined above, and without the limitations of paragraphs (a)-(d), is new.