Extracurricular laboratory: Synthetic route of 2,5-Dichloronicotinic acid

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,59782-85-3, its application will become more common.

Related Products of 59782-85-3 ,Some common heterocyclic compound, 59782-85-3, molecular formula is C6H3Cl2NO2, 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.

Preparation of 5-chloro-2-morpholino-pyridine-3-carboxylic acid: to a solution of 2,5-dichloropyridine-3-carboxylic acid (50 mg, 0.26 mmol, 1 eq) in NMP (300 mu,) was added morpholine (250 mu,, 2.6 mmol, 10 eq). The reaction mixture was stirred at 100 C for 1 h. The mixture was poured into water and made acid with 1 M HCl, extracted with EtOAc to yield 5-chloro-2-morpholino-pyridine-3-carboxylic acid. The crude compound contained NMP and was used in the next step without purification. LCMS: (M+H) = 243, UV = 96 % pure. 1H NMR (300 MHz, DMSO-d6) delta 8.30 (d, J= 2.6 Hz, 1H), 7.95 (d, J= 2.6 Hz, 1H), 3.66 (dd, J= 5.5, 3.8 Hz, 4H), 3.41 – 3.35 (m, 4H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,59782-85-3, its application will become more common.

Reference:
Patent; NUEVOLUTION A/S; GERNER SEITZBERG, Jimmi; TITILOLA AKINLEMINU KRONBORG, Tine; POLJAK, Visnja; FRIBERG, Gitte; TEUBER, Lene; (487 pag.)WO2016/16316; (2016); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem