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6-chloro-5-iodopyrazin-2-amine synthesis
- Product Name:6-chloro-5-iodopyrazin-2-amine
- CAS Number:925678-00-8
- Molecular formula:C4H3ClIN3
- Molecular Weight:255.44
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33332-28-4
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925678-00-8
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Yield: 88%
Reaction Conditions:
with N-iodo-succinimide in dimethyl sulfoxide at 25;
Steps:
32.a A. 6-Chloro-5-iodopyrazin-2-amine
To a solution of 6-chloropyrazin-2-amine (10 g, 77.2 mmol) in DMSO (100 mL) was added NIS (17.4 g, 77.2 mmol) and the solution was stirred at 25°C overnight. After the mixture was poured into water and extracted with EtOAc, the organic solutions were collected, washed with brine, dried over NaS04 and filtered. The filtrate was evaporated under reduced pressure and the residue purified by silica gel chromatograph using Petroleum Ether:EtOAc 1 :4 as eluting solvents to afford 6-chloro-5-iodopyrazin-2-amine as a yellow solid (17.2 g, 88%). MS (ESI) m/z: 255 [M+H]+.
References:
BEAUFOUR IPSEN TIANJIN PHARMACEUTICAL CO., LTD;AUVIN, Serge;LAVERGNE, Olivier;CHAO, Qi;CHEN, Yufeng WO2015/100609, 2015, A1 Location in patent:Page/Page column 52; 53