| 摘要 |
1289137 Pyrido[2,3-d]pyrimidin-2-ones SANDOZ Ltd 1 Dec 1969 [10 Dec 1968] 58488/69 Heading C2C The invention comprises compounds of formula wherein x-y is CR 2 =N or CHR 2 -NH, R is H or C 1-5 alky], R 1 is C 1-6 alkyl, C 3-6 cycloalkyl, allyl, methallyl or propargyl, and R 2 is Ph possibly containing 1-2 substituents which are F, Cl, Br, C 1-4 alkyl or C 1-4 alkoxy. These compounds are prepared by (1) reacting the corresponding precursor in which R, is an alkali metal atom, with R 1 X (R 1 #tertiary alkyl; X=Cl, Br or I); (2) reacting a (possibly RStibstituted) 2 - R 1 NH - 3 - pyridyl/phenyl ketimine with COCl 2 , ClCO 2 Me, ClCO 2 Et. NH 1 CO 2 -alkyl (C 1-5 ) at not less than 140‹ C. or 1,1<SP>1</SP>- carbonyldiimidazole (but only compounds when R 1 =tertiary alkyl); (3) reacting a (possibly R-substituted) 2-R 1 NH-3-benzoylpyridine (R 1 #tertiaty alkyl) with urea or isocyanic acid, or with NH 2 CO 2 -alkyl (C 1-5 ) at not less than 140‹ C. in presence of a Lewis acid; (4) (further 3,4-dihydro-compounds) reducing the non-hydrogenated analogue in an inert organic solvent. Starting materials.-Details are given for the preparation of 2-chloro-6-methyl-nicotinonitrile, and 2-isopropylaminonicotinonitrile and its 6- methyl derivative. Therapeutic compositions: for oral or parenteral administration comprise compounds of the above formula, which have anti-inflammatory activity. |
