发明名称 Substituted pyrazines and a process for producing the same
摘要 Described include (1) a substituted pyrazine compound of general formula (VIII):; and (2) a process for producing the substituted pyrazine compound of general formula (VIII), where R1 is hydrogen, a halogen, a substituted or unsubstituted hydrocarbon group, or a substituted or unsubstituted heterocyclic group, and R4 is a protecting group. The process comprises (1) the step of reacting 2-amino-3,5-dibromo-6-chloropyrazine with R1MgX and ZnCl2 in the presence of a palladium catalyst to produce a compound of general formula (V); (2) the step of reacting the compound of general formula (V) with a compound of general formula (VI) to produce a compound of general formula (VII); and (3) the step of reacting the compound of formula (VII) with tributyl(vinyl)tin in the presence or a palladium catalyst to given the compound of general formula (VIII).
申请公布号 US9346767(B2) 申请公布日期 2016.05.24
申请号 US201514734471 申请日期 2015.06.09
申请人 JNC CORPORATION;NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY 发明人 Inouye Satoshi;Miura Yuiko;Yoshida Suguru;Hosoya Takamitsu
分类号 C07D241/20;C07D241/38;C07D241/44;C07D487/04;C07D241/54 主分类号 C07D241/20
代理机构 Drinker Biddle & Reath LLP 代理人 Drinker Biddle & Reath LLP
主权项 1. A compound represented by formula (VIII): wherein R1 is hydrogen; a halogen; an aryl which may optionally be substituted with at least one substituent selected from the group consisting of a halogen, hydroxy, an alkyl having 1 to 6 carbon atoms, an alkoxy having 1 to 6 carbon atoms, an amino and a dialkylamino having 1 to 6 carbon atoms; an arylalkyl which may optionally be substituted with at least one substituent selected from the group consisting of a halogen, hydroxy, an alkyl having 1 to 6 carbon atoms, an alkoxy having 1 to 6 carbon atoms, an amino and a dialkylamino having 1 to 6 carbon atoms; an arylalkenyl which may optionally be substituted with at least one substituent selected from the group consisting of a halogen, hydroxy, an alkyl having 1 to 6 carbon atoms, an alkoxy having 1 to 6 carbon atoms, an amino and a dialkylamino having 1 to 6 carbon atoms; an alkyl which may optionally be substituted with an alicyclic group; an alkenyl which may optionally be substituted with an alicyclic group; an alicyclic group; a heterocyclic group; or an alkynyl which may optionally be substituted with an alicyclic group, and R4 is a protecting group selected from the group consisting of methyl, methoxymethyl, tetrahydropyranyl, benzyl, 4-methoxybenzyl, tert-butyldimethylsilyl, trimethylsilyl, triethylsilyl, phenyldimethylsilyl, tert-butyldiphenylsilyl, and triisopropylsilyl.
地址 Tokyo JP