PROCESS FOR THE PRODUCTION OF COMPOUNDS HAVING 5- TO 10-MEMBERED AROMATIC HETEROCYCLES WITH ALKYLMAGNESIUM MONOAMIDES

摘要

The invention aims at providing an anionizing agent for heteroaromatic compounds which has the following advantages: (1) the reactivity (degree of anionization) is high, (2) the reaction can be conducted at relatively high temperatures and the formed anion is stable at the relatively high temperatures, (3) the formation of by-products is inhibited, and (4) the safety is satisfactory even in the use on an industrial scale; and a process for the production of heteroaromatic compounds which comprises converting a heteroaromatic compound into an anion by the use of the anionizing agent and reacting the anion with an electrophile to conduct electrophilic substitution. The above aim is attained by reacting a compound having a 5- to 10-membered aromatic heterocycle which may have one to three substituents (such as R10), e.g., a compound [(2)-4’] with a compound represented by the general formula (1) (wherein R1 is C1-6 alkyl; A1 is a group represented by the general formula: -NR2R3 or the like; and R2 and R3 are each C1-6 alkyl having piperazinyl or di(C1-6 alkyl)amino) and reacting the obtained anion with an electrophile. (X)