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专利信息

专利号:WO-2022190047-A1
优先权日:2021-03-12
标题:Process for consecutive continuous-flow reductions in the synthesis of medicinally relevant piperazine derivatives using a tubular reactor with alternating diameter
发明人：BANA PÉTER; FÃœLÖP ZSOLT; ÉLES JÃ?NOS
权利人:RICHTER GEDEON NYRT
摘要:The present invention relates to a novel alternating diameter flow reactor for continuous - flow reactions, a system for continuous-flow reactions (as shown in Figure 1) comprising said alternating diameter flow reactor, a method for the formation of the C-N bond carried out in said system and a process for the preparation of the antipsychotic drug cariprazine described by the chemical structure (I) and its intermediates, and as well as other related 1-arylpiperazine active pharmaceutical ingredients conducted in two continuous-flow reactors of said system comprising the consecutive steps of a first step being selective ester reduction carried out in said alternating diameter flow reactor and a second step being reductive amination carried out by continuous-flow catalytic hydrogenation.