Reference of 36070-80-1, A common heterocyclic compound, 36070-80-1, name is 5-Chloropyrazine-2-carboxylic acid, molecular formula is C5H3ClN2O2, its 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.
Example 56 2 (R)- (3-CHLORO-4-METHANESULFONYL-PHENYL)-3-CYCLOPENTYL-N- [5- (2-HYDROXY-1- HYDROXYMETHYL-ETHOXY)-PYRAZIN-2-YL]-PROPIONAMIDE [000288] A suspension of 5-chloro-pyrazine-2-carboxylic acid (prepared as in Example 29,1. 00 g, 6.33 mmol) in methylene chloride (30 mL) was treated with 1,3- dibenzyloxy-2-propanol (2.06 g, 7.57 MMOL), bis (2-oxo-3-oxazolidinyl) phosphinic chloride (1.61 g, 6.34 mmol), and triethylamine (1.83 mL, 12.66 mmol). The mixture was stirred at 25C overnight. The solution was extracted with methylene chloride and a saturated sodium bicarbonate solution. The organic layer was washed with water, a saturated aqueous sodium chloride solution, a 1N hydrochloric acid solution and a saturated aqueous sodium chloride solution. The organic layer was dried over sodium sulfate, filtered, and concentrated in vacuo. Biotage chromatography (FLASH 40L, Silica, 3/1 hexanes/ethyl acetate) afforded the 5-chloropyrazine-2-carboxylic acid 2- BENZYLOXY-1-BENZYLOXYMETHYL-ETHYL ester (1.45 g, 55.7%) as a colorless oil.
The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; WO2004/52869; (2004); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem