2,5-DibroMo-4-MethylpyriMidine

Sodium hydride (0.128g, 60% disp. in oil) was added to a stirred solution of 2-methyl- 1, 2, 5-thiadiazolidine 1, 1-dioxide (0.433g) in THF (10ml). DMF (10ml) was added and the mixture heated at 80C for 5min then a solution of the product from step (i) (0.8g) in DMF (SML) was added. The mixture was heated at 60C for 10MIN, poured into water (100ml), acidified with citric acid and extracted with ethylacetate. The organics were evaporated under reduced pressure and the residue purified by chromatography on silica eluting with diethylether, yield 0.58g. 1H NMR CDC13 : 8 8.50 (s, 1H), 4.05 (t, 2H), 3.45 (t, 2H), 2.87 (s, 3H), 2.58 (s, 3H). MS: APCI (+ve) 307/9Isoamylnitrite (21ML) was added to a stirred suspension of 5-bromo-4-methyl-2- PYRIMIDINAMINE (1.75g) in bromoform (30ML) and the mixture heated at 85°C for 4h. After cooling, isohexane (300ML) was added and the solution passed through a pad of silica-gel. The silica was washed with petrol (1000ml), dichloromethane (200ml) then the product eluted with ethylacetate. The ethylacetate layer was evaporated under reduced pressure and the residue purified by chromatography on silica eluting with 5percent diethylether/ isohexane, yield 0. 9g 1H NMR CDC13 : No. 8. 52 (s, 1H), 2.64 (s, 3H) MS: APCI (-VE) 249/51/53A mixture of the product from example 135 step (i) (0. 75G), AZETIDIN-3-OL hydrochloride (0.66g) and triethylamine (0. 9ml) in ethanol (10ml) was stirred at RT for 2h. The solvent was removed under reduced pressure and the residue purified by chromatography on silica eluting with 60% diethylether/isohexane as eluant, yield 0.7g. 1H NMR CDC13 : 88. 22 (s, 1H), 4.78-4. 72 (m, 1H), 4.40-4. 33 (m, 2H), 3.99-3. 93 (m, 2H), 2.45 (s, 3H)

Molecular Weight:251.91
XLogP3:2.3
Hydrogen Bond Acceptor Count:2
Exact Mass:251.87207
Monoisotopic Mass:249.87412
Topological Polar Surface Area:25.8
Heavy Atom Count:9
Complexity:99
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes