2-AMINO-5-ETHYLPYRAZINE

Step 1: 28.7 g (165 mmol) of 5-bromopyrazin-2 -amine and 1.78 g (3.28 mmol) of [1 , 3- bis(diphenylphosphino)propane]dichloronickel(ll) are suspended in 400 ml of dioxane at room temperature under argon. 300 g of a 15 wtpercent-solution (1 .1 M) of diethylzinc in toluene are slowly added at 12°C during 90 minutes giving a turbid brown solution. The reaction temperature is raised to 21 °C during one hour and the reaction completed by stirring at 21 °C for an 90 minutes. 30 ml of methanol are slowly added by controlling the temperature to 21 °C by cooling. The resulting solution is concentrated under vacuum and further suspended in 600 ml of toluene fol- lowed by the addition of 50 g of HyfloA mixture of the compound (1.40 g) obtained in Reference Example 434 and 10percent palladium carbon (1.40 g) in methanol (45.0 mL) was stirred under a hydrogen atmosphere at room temperature for 3 h A mixture of the compound (1.40 g) obtained in Reference Example 434 and 10% palladium carbon (1.40 g) in methanol (45.0 mL) was stirred under a hydrogen atmosphere at room temperature for 3 h The reaction mixture was filtered through diatomaceous earth and concentrated to give the title compound (1.40 g). MS(ESI)m/z; 124[M+H]+Pyridine (1.051 mL, 12.99 mmol) was added dropwise to a stirred solution of phenyl carbonochloridate (1.324 mL, 10.56 mmol) in dichloromethane (DCM) (20 ml) at room temperature and stirred for 30 minutes. Then Pyridine (1.051 mL, 12.99 mmol) was added dropwise to a stirred solution of phenyl carbonochloridate (1.324 mL, 10.56 mmol) in dichloromethane (DCM) (20 ml) at room temperature and stirred for 30 minutes. Then To a solution of (4S)-7-(6-methylpyridin-3-yl)-2, 3, 4, 5-tetrahydro-1, 4-methanopyrido[2, 3-b][1, 4]diazepine (600 mg, 2.378 mmol), triphosgene (706 mg, 2.378 mmol) and triethylamine (1.989 mL, 14.27 mmol) in tetrahydrofuran (THF) (15 mL) stirred under nitrogen at room temperature for 30 min was added To a solution of (4S)-7-(6-methylpyridin-3-yl)-2, 3, 4, 5-tetrahydro-l, 4-methanopyrido[2, 3- b][l, 4]diazepine (600 mg, 2.378 mmol), triphosgene (706 mg, 2.378 mmol) and triethylamine (1.989 mL, 14.27 mmol) in tetrahydrofuran (THF) (15 mL) stirred under nitrogen at room temperature for 30 min was added 21.0 g (0.171 mol) of

Molecular Weight:123.16
XLogP3:0.3
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:1
Exact Mass:123.079647300
Monoisotopic Mass:123.079647300
Topological Polar Surface Area:51.8
Heavy Atom Count:9
Complexity:84.4
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes