Reference of 122-05-4,Some common heterocyclic compound, 122-05-4, name is Pyrazine-2,5-dicarboxylic acid, molecular formula is C6H4N2O4, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Step 1: To a solution of { (S)-1 – [(S)-1 -(6-bromo-2-methoxy-naphthalen- 1 -ylmethyl)-2- oxo-2,3 ,4,5-tetrahydro- 1 H-benzo [b] [1,4] diazepin-3-ylcarbamoyl] -ethyl } -methyl-carbamic acid tert-butyl ester (Intermediate 11) (300 mg, 0.49 mmol) and pyrazine-2,5-dicarboxylic acid (41.2mg, 0.24 mmol) in pyridine (5 mL) at 0 C was added POC13 (46 tL, 0.49mmol) and the cooling bath removed. After 5 h, the mixture was diluted with dichloromethane, washed with water, dried (Na2504) and concentrated. The residue was purified by preparative reverse phase HPLC to afford tert-butyl N- [(1 S)-2- [[(35)-5- [(6-bromo-2-methoxy- 1 -naphthyl)methyl] -1- [5-[(35)-5- [(6-bromo-2-methoxy- 1 -naphthyl)methyl] -3- [[(2S )-2- [tert15 butoxycarbonyl(methyl)amino]propanoyl] amino] -4-oxo-2,3-dihydro- 1,5 -benzodiazepine- 1-carbonyl]pyrazine-2-carbonyl] -4-oxo-2,3-dihydro- 1,5 -benzodiazepin-3-yl] amino] -1 -methyl-2- oxo-ethyl]-N-methyl-carbamate (52 mg, 7.82 %) as an off white solid. LC-MS: 1355.0 (M+H).
The synthetic route of 122-05-4 has been constantly updated, and we look forward to future research findings.