8 Sep 2021 News Introduction of a new synthetic route about 62802-42-0

With the rapid development of chemical substances, we look forward to future research findings about 62802-42-0.

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 62802-42-0, name is 2-Chloro-5-fluoropyrimidine, molecular formula is C4H2ClFN2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. category: pyrimidines

To a solution of 2- chloro-5-fluoropyrimidine (10.0 g, 75.46 mmol, Sigma Aldrich) in DMF (100 mL) was added tributyl(vinyl)tin (31.1 g, 98.09 mmol) at RT. The reaction mixture was purged with N2for 5 min and Pd(PPh3)4(2.62 g, 2.26 mmol) was added. The reaction mixture was further degassed with N2for 5 min and stirred at 100 C for 24 h. After completion of the reaction (monitored by TLC), the reaction mixture was cooled to RTand quenched with water (100 mL). The aqueous layer was extracted with diethyl ether (2 x 100 mL) and the combined organic layers were washed with brine (100 mL), dried over anhydrous Na2SO4, and concentrated in vacuo to obtain the initial product which was purified by silica gel chromatography (eluent: 6% EtOAc in hexanes) to provide 400.1 (8.0 g, 85% yield) as an oil.1H NMR (400 MHz, CDCl3) delta 8.58- 8.49 (m, 2H), 6.86 (dd, J = 17.4, 10.6 Hz, 1H), 6.53 (d, J = 17.3 Hz, 1H), 5.70 (d, J = 10.6 Hz, 1H). LCMS-ESI (pos.) m/z: = 125.1.

With the rapid development of chemical substances, we look forward to future research findings about 62802-42-0.

Reference:
Patent; AMGEN INC.; CHEN, Ning; CHEN, Xiaoqi; CHEN, Yinhong; CHENG, Alan C.; CONNORS, Richard V.; DEIGNAN, Jeffrey; DRANSFIELD, Paul John; DU, Xiaohui; FU, Zice; HARVEY, James S.; HEATH, Julie Anne; HEUMANN, Lars V.; HORNE, Daniel B.; HOUZE, Jonathan; KALLER, Matthew R.; KAYSER, Frank; KHAKOO, Aarif Yusuf; KOPECKY, David J.; LAI, Su-Jen; MA, Zhihua; MEDINA, Julio C.; MIHALIC, Jeffrey T.; NISHIMURA, Nobuko; OLSON, Steven H.; PATTAROPONG, Vatee; SWAMINATH, Gayathri; WANG, Xiaodong; WANSKA, Malgorzata; YANG, Kevin; YEH, Wen-Chen; (700 pag.)WO2018/97945; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia