作者: Lianhe Shu , Ping Wang , Chen Gu , Lisa Garofalo , Lady Mae Alabanza
DOI: 10.1021/OP300270R
关键词:
摘要: A concise synthesis of a tetrahydropyrazolopyrazine building block is described. 5-Methyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-ylamine was prepared in three steps and 80% yield from 5-nitro-2H-pyrazole-3-carboxylic acid. This compound then coupled with 4-bromo-6-chloro-2-methyl-2H-pyridazin-3-one the presence sodium tert-pentoxide to give target product 87% yield. The process successfully scaled up multihundred gram scale.