Microwave-assisted solid-phase synthesis of a 1,2-disubstituted benzimidazole library by using a phosphonium linker

Ríos N.; Chavarría C.; Gil C.; Porcal W.

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Microwave-assisted solid-phase synthesis of a 1,2-disubstituted benzimidazole library by using a phosphonium linker

机译：a连接基的微波辅助固相合成1,2-二取代苯并咪唑库

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An efficient and rapid microwave-assisted solid-phase method for the synthesis of 5-methyl-1,2-disubstituted benzimidazoles derivatives has been developed. The phosphonium linker, obtained by reaction between polymer-supported triphenylphosphine and 4-fluoro-3-nitrobenzyl iodide, underwent aromatic substitution with primary amines, followed by one-pot reaction with aldehydes in the presence of SnCl_2·2H _2O, yielded the benzimidazole system under microwave irradiation. The final products were released from the resin with NaOH under microwave irradiation and were obtained in high purity and good overall yield.

机译：已经开发了一种高效且快速的微波辅助固相法，用于合成5-甲基-1，2-二取代的苯并咪唑衍生物。通过聚合物负载的三苯基膦与4-氟-3-硝基苄基碘的反应获得的phospho连接基，用伯胺进行芳族取代，然后在SnCl_2·2H_2O的存在下与醛进行一锅反应，生成苯并咪唑体系在微波照射下。在微波辐射下用NaOH从树脂中释放出最终产物，并以高纯度和良好的总收率获得。

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《Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry》 |2013年第3期|共7页
作者
Ríos N.; Chavarría C.; Gil C.; Porcal W.;
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正文语种 eng
中图分类有机化学;
关键词
rapid microwave-assisted; solid-phase; 5-methyl-1; 2-disubstituted;

机译：快速微波辅助;固相;5-甲基-1;2-二取代;

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1. Microwave-assisted solid-phase synthesis of a 1,2-disubstituted benzimidazole library by using a phosphonium linker [J] . Ríos N., Chavarría C., Gil C., Journal of Heterocyclic Chemistry: The International Journal of Heterocyclic Chemistry . 2013,第3期

机译：a连接基的微波辅助固相合成1,2-二取代苯并咪唑库
2. Metal-free selective synthesis of 2-substituted benzimidazoles catalyzed by Bronsted acidic ionic liquid: Convenient access to one-pot synthesis of N-alkylated 1,2-disubstituted benzimidazoles [J] . Senapak Warapong, Saeeng Rungnapha, Jaratjaroonphong Jaray, Tetrahedron . 2019,第26期

机译：无金属选择性合成2-取代的苯并咪唑催化的铜酸性离子液体：方便进入N-烷基化1,2-二取代苯并咪唑的单罐合成
3. Microwave-Assisted Synthesis of Benzimidazole-Linked Indoline and Indole Hybrids from C-2 Linked (o-Aminobenzyl)benzimidazoles [J] . Lee Yun-Ta, Chiu Feng-Yu, Barve Indrajeet J., Advanced synthesis & catalysis . 2018,第3期

机译：微波辅助合成苯并咪唑与吲哚吲哚和吲哚杂交物联合的C-2连接（O-氨基苄基）苯并咪唑
4. Selective Synthesis of 2-Substityted and 1,2-Disubstituted Benzimidazoles [C] . Chengjun Wang, Shanshan Gong, Qi Sun International Conference on Material Engineering, Chemistry, Bioinformatics . 2014

机译：选择性合成2-Coffallated和1,2-二取代的苯并咪唑
5. A photolabile backbone amide linker for the solid-phase synthesis of cyclic peptides. Cysteine-free native chemical ligation. Synthesis and biological evaluation of a library of resveratrol analogues. [D] . Kang, Soo Sung. 2009

机译：光不稳定的主链酰胺接头，用于固相合成环状肽。无半胱氨酸的天然化学连接。白藜芦醇类似物文库的合成和生物学评估。
6. Microwave-Assisted Synthesis of Mono- and Disubstituted 4-Hydroxyacetophenone Derivatives via Mannich Reaction: Synthesis XRD and HS-Analysis [O] . Ghadah Aljohani, Musa A. Said, Dieter Lentz, 2019

机译：曼尼希反应的微波辅助合成单和双取代的4-羟基苯乙酮衍生物：合成XRD和HS分析
7. Microwave-assisted solid-phase synthesis of a 1,2-disubstituted benzimidazole library by using a phosphonium linker [O] . Ríos N., Chavarría Cecilia, Gil Carmen, 2013

机译：a连接基的微波辅助固相合成1,2-二取代苯并咪唑库
8. Organolithium Routes to 1,2-Disubstituted Ethylene Derivatives. An Attempted Synthesis of 1,2-Dilithioethylene. [R] . Seyferth, D., Vick, S. C. 1977

机译：有机锂路由到1,2-二取代乙烯衍生物。试图合成1,2-二硫代乙烯。

Microwave-assisted solid-phase synthesis of a 1,2-disubstituted benzimidazole library by using a phosphonium linker

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