6-BroMo-3-iodo-8-Methylsulfanyl-iMidazo[1,2-a]pyrazine synthesis

Yield: 96%

Reaction Conditions:

with N-iodo-succinimide in N,N-dimethyl-formamide at 60; for 6.5 h;Inert atmosphere;

Steps:

2
Intermediate Example 26-Bromo-3-iodo-8-(methylsulfan l)imidazo[1 ,2-a]pyrazineTo a solution of 5.23 g (21 .4 mmol) 6-Bromo-8-(methylsulfanyl)imidazo[1 ,2- a]pyrazine which was prepared according to Intermediate Example 1 , supra, in 142 mL Ν,Ν-dimethylformamide were added 5.06 g N-iodosuccinimide and the mixture was stirred at 60° C for 6.5 hours. Most of the solvent was removed under reduced pressure, water was added and the residue extracted with dichloromethane. The organic phase was washed with water, aqueous sodium thiosulfate and dried over sodium sulfate. After filtration and removal of the solvent 7.61 g (96%) of the title compound were isolated that were used without further purification.

References:

BAYER PHARMA AKTIENGESELLSCHAFT;KLAR, Ulrich;KOPPITZ, Marcus;KOSEMUND, Dirk;BOHLMANN, Rolf;BADER, Benjamin;LIENAU, Philip;SIEMEISTER, Gerhard;PRECHTL, Stefan;NGUYEN, Duy;SCOTT, William WO2011/113862, 2011, A1 Location in patent:Page/Page column 55-56