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2-氨基-3-硝基吡啶置于氢溴酸,Sodium Nitrite,Copper(I) Bromide体系中,化学反应生成2-溴-3-硝基吡啶
参考文献:新型卤代吡啶基硼酸和酯的合成.第2部分:2,4或5-卤代吡啶-3-基硼酸和酯
标题:新型卤代吡啶基硼酸和酯的合成.第2部分:2,4或5-卤代吡啶-3-基硼酸和酯
摘要:本文描述了用于合成和5-卤代吡啶-3-基-硼酸酯的一般方法的新的2,4-隔离,或和4,7,10,13,15.这些化合物的制备考虑了使用n Buli进行的区域选择性卤素-金属交换或区域选择性邻位交换-使用二异丙基氨基锂进行锂化,然后从适当的单或二卤代吡啶开始,用硼酸三异丙基酯淬灭.迄今为止研究的所有底物均提供单一的区域异构硼酸或酯产物.另外,已经发现这些化合物与一系列的芳基卤化物进行了pd催化的偶联,并授权了一种制备新吡啶文库的策略.
Doi:10.1016/s0040-4020(02)00283-1

专利信息

专利号:US-8735586-B2
优先权日:2007-06-26
标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
发明人：ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR
权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

专利号:EP-2173747-B1
优先权日:2007-06-26
标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
发明人：ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS
权利人:SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

专利号:US-2010261909-A1
优先权日:2007-06-26
标题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles

专利号:WO-2009000413-A1
优先权日:2007-06-26
标题:A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles

专利号:CA-2693142-A1
优先权日:2007-06-26
标题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles

专利号:AU-2008267444-A1
优先权日:2007-06-26
标 题 :A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles