6-Bromo-3-chloropyrazin-2-amine synthesis

Yield: 66%

Reaction Conditions:

with ammonium hydroxide at 100;Sealed tube;

Steps:

90.E E. 6-Bromo-3-chloropyrazin-2-amine, 90e
[0955] Into a 250 mL sealed tube was placed compound90d (50.0 g, 184 mmol) andNH40H (150mL). The resultingmixture was stirred overnight at 100° C. Uponcooling, a solidwas collected by filtration and dried in an oven under reducedpressure to obtain the compound 90e as a grey solid (28.0 g,66% yield), which was used in next step without furtherpurification.

References:

JANSSEN PHARMACEUTICA, NV;Player, Mark R.;Meegalla, Sanath K.;Illig, Carl R.;Chen, Jinsheng;Wilson, Kenneth J.;Lee, Yu-Kai;Parks, Daniel J.;Huang, Hui;Patel, Sharmila;Lu, Tianbao US2014/364414, 2014, A1 Location in patent:Paragraph 0945; 0954-0955