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20th February 2014 @ 03:56


6-Chloropyrazine-2-carboxylic acid (300 mg, 1.89 mmol, 1 eq.), 3-chloro-2-fluoroaniline (0.21 mL, 1.89 mmol, 1 eq.) and DIEA (0.66 ml, 3.78 mmol, 2 eq.) were stirred in DMF (1.8 mL) at 0 ˚C. T3P (50 % by wt in EtOAc,  1.5 eq.) was added dropwise at 0 ˚C. The reaction mixture was stirred for 15 min at this temperature and then allowed to reach room temperature. The mixture was left stirring for 18 h. A TLC and NMR of a mini work up showed that the reaction had not gone to completion. Thus, more T3P (1 mL, 50 % by wt in EtOAc, 1.70 mmol) was added at 0 ˚C to the reaction mixture and it was left to stir at room temperature over the weekend..

Hazard Assessment

Synthesis of IT 5 6-chloro-N-(3-chloro-2-fluorophenyl)pyrazine-2-carboxamide.docx

InChI

InChI=1S/C5H3ClN2O2/c6-4-2-7-1-3(8-4)5(9)10/h1-2H,(H,9,10)

and

InChI=1S/C6H5ClFN/c7-4-2-1-3-5(9)6(4)8/h1-3H,9H2

to

InChI=1S/C11H6Cl2FN3O/c12-6-2-1-3-7(10(6)14)17-11(18)8-4-15-5-9(13)16-8/h1-5H,(H,17,18)

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Attached Files
Synthesis of IT 5-1 6-chloro-N-(3-chloro-2-fluorophenyl)pyrazine-2-carboxamide.png
Synthesis of IT 5 6-chloro-N-(3-chloro-2-fluorophenyl)pyrazine-2-carboxamide.docx