连续的异腈多组分/氮杂Wittig反应合成具有生物活性的氮杂环
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摘要
含氮杂环化合物由于其广谱、高效、低毒等优良的生物活性而备受化学家的关注,如在杀虫、杀菌、除草、抗病毒、消炎和抗肿瘤等领域都表现出较好的发展前景。已有许多含氮杂环化合物被开发成医药和农药新品种,国内外关于新型含氮杂环类化合物的合成及生物活性的研究十分活跃。本文应用连续的IMCR/Staudinger/aza-Wittig反应,设计并合成了4位酰氨基取代的4H-3,1-苯并噁嗪类化合物、3,4-二氢-2,3,4-三取代喹唑啉类化合物和吲哚并[1,2-c]喹唑啉类化合物。并将1,2,4-三唑活性基团引入到Ugi反应产物的分子构架中,设计合成了新型1,2,4-三唑衍生物；以烯唑醇为先导化合物,将烯唑醇链状化合物结构骨架设计到杂环分子中,应用Friedlander反应合成了新型3-唑基喹啉衍生物。研究了目标化合物的合成条件、反应机理和波谱性质,并对部分化合物进行了抑菌活性测试。具体内容如下：
1.就最近几年来IMCR在杂环合成中的应用及aza-Wittig反应的最新进展进行了系统综述,并对三唑类杀菌剂和咪唑类杀菌剂进行了简单介绍。
2.应用连续的Passerini/Staudinger/aza-Wittig反应合成了4位酰氨基取代的4H-3,1-苯并噁嗪类化合物,对其反应规律、化合物性质进行了研究和讨论；对实验中丙酮酸的引入所产生的异常现象进行了解释,并通过膦亚胺与异氰酸酯的分子间aza-Wittig反应,经由碳二亚胺和分子内亲核加成,同样得到了4位酰氨基取代的4H-3,1-苯并噁嗪类化合物。为该类化合物的合成提供了新方法,该方法不仅原料易得,而且操作简单、条件温和、产率较高。合成路线如下：(?)
3.运用连续的Ugi/Staudinger/aza-Wittig反应来合成了3,4-二氢-2,3,4-三取代喹唑啉类化合物,并通过IR.1HNMR、13CNMR、MS和元素分析对目标化合物结构进行了表征,研究了其波谱性质。培养了其中一个代表性化合物的单晶,对该类化合物结构进一步进行确证和分析,通过对目标化合物分子结构的分析提出了可能的反应机理。这是第一例报道N,N-二取代的酰胺(无NH)可与碳二亚胺活性碳原子发生加成反应,反应过程中发生酰基重排而得到3,4-二氢喹唑啉衍生物,并对其中取代基对反应的影响进行了研究。合成路线如下：(?)
4.由异腈、羧酸、2-羰基苯胺和2-叠氮基苯甲醛出发,经连续的Ugi/Staudinger/aza- Wittig反应,得到了吲哚并[1,2-c]喹唑啉类化合物,采用IR、1HNMR、13CNMR、MS和元素分析等方法对目标化合物的结构进行了表征,讨论了其波谱性质。并通过其中一个代表性化合物的X-Ray单晶衍射分析,对该类化合物的结构进一步进行了确证。通过对目标化合物分子结构的分析提出了可能的反应机理,首次报道了Ugi反应产物中的次甲基碳对羰基的亲核加成得到吲哚化合物,讨论了取代基对反应的影响,并通过对照实验验证了其中喹唑啉环与吲哚环的形成是连续进行的。合成路线如下：(?)
5.将1,2,4-三唑环活性基团引入到Ugi反应产物的分子构架中,设计合成了新型的1,2,4-三唑化合物；并以烯唑醇为先导化合物,将烯唑醇链状化合物结构骨架设计到杂环分子中,应用Friedlander反应合成了新型3-唑基喹啉衍生物。具体路线如下：(?) (?)
6.在浓度为50 ppm时,对部分目标化合物进行了柑橘绿霉菌的抑菌活性测试,初步筛选结果表明部分化合物具有一定的抑制活性,如化合物30n对柑橘绿霉菌的抑制率达到90%。进一步活性测试发现,该化合物在10 ppm时,对小麦颖枯病仍然具有99%的防效。(?) 30n
Chemists have expressed great concern about N-heterocycles because of their good biological activities, such as broad-spectrum, efficient and low toxicity. The study of N-heterocycles chemistry have found a great deal of compounds with good prospects in pesticide、fungicide、herbicide、anti-Virus、anti-inflammatory and anti-tumor drugs. Some of them have been used as pesticide and medicine, the research on the synthesis and evaluate their biological activities of new N-heterocycle compounds is very active. In this dissertation we applied sequential IMCR/Staudinger/aza-Wittig reaction to design and synthesize 4-aminocarbonyl substituted 4H-3,1-benzoxazines,3,4-dihydro-2,3,4-trisubstitued quinazolines and indolo[1,2-c]quinazolines. And a series of unreported 1,2,4-triazole derivatives were designed and synthesized using Ugi reaction with the aim of evaluating their biological activities. Furthermore, novel 3-azolyl-quinoline derivatives were designed and synthesized using Friedlander reaction based on the lead compound "Diniconazole", a commercial triazole fungicide. The conditions of the syntheisis and the mechanism of the reaction were discussed, and the spectral properties of the target molecules were researched. The fungicidal activities of partial compounds were also tested. It may be summarized as follows:
1. The utilization of IMCR in the synthesis of heterocycles and the development of aza-Wittig reaction of recent years were reviewed, and a few commercial fungicides of triazole derivatives and imidazole derivatives were briefly introduced.
2.4-Aminocarbonyl substituted 4H-3,1-benzoxazine derivatives were synthesized using sequential Passerini/Staudinger/aza-Wittig reaction. The synthetic conditions and properties of the target compounds were studied and discussed. The unexpected phenomena of the reaction while pyruvic acid was used in the Passerini reaction were explained, and using further intermolecular aza-Wittig reaction via iminophosphoranes and isocyanates also give 4-aminocarbonyl substituted 4H-3,1-benzoxazine derivatives through carbodiimides and nucleophilic addition reaction. The synthetic routes could be used as new method to construct 4H-3,1-benzoxazines not only due to the easily accessible starting materials, but also for the simple operation, mild reaction conditions and the high yields. Following are the synthetic routes. (?) (?)
3.A series of 3,4-dihydro-2,3,4-trisubstitued quinazoline derivatives were synthesized using sequential Ugi/Staudinger/aza-Wittig reaction,and the structures of the target compounds were characterized via IR,1HNMR,13CNMR,MS and elemental analysis,and the spectral properties were also studied.Furthermore,the structure of the qninazoline derivatives was further confirmed and analysised through X-Ray single crystal diffraction by one representative compound.Through the structure analysis of the target molecules,a possible mechanism for the formation of the 3,4-dihydroquinazolines is proposed.It is the first report that N,N-disubstituted amides(containing no N-H moiety)could react with carbodiimides,and 3,4-dihydroquinazolines were formed through the further rearrangement of acyl group.The influence on the reaction of substituents was also studied, and following is the synthetic route. (?)
4.A sequential Ugi/Staudinger/aza-Wittig/nucleophilic addition reaction was developed to construct indolo[1,2-c]quinazoline derivatives,starting from carboxylic acid,2-azidobenzaldehyde, 2-acylaniline and isocyanide.And the structures of the compounds were characterized through IR, 1HNMR,13CNMR,MS and elemental analysis,the spectral properties were also discussed.The structure of the indolo[1,2-c]quinazoline derivatives was further established through X-Ray single crystal diffraction by one representative compound.Through the structure analysis of the target molecules,a possible mechanism for the formation of indolo[1,2-c]quinazolines is proposed.And this is the first report of the cyclization of the Ugi adduct to give indole ring system via the nucleophilic addition reaction of the methine group to the carbonyl group. Furthermore, the influence of substituents on the reaction was studied,and it is confirmed that the quinazoline ring together with the indole ring were formed sequentially through controlled reactions.Following is the synthetic route. (?)
5.A series of unreported 1,2,4-triazole derivatives were designed and synthesized using Ugi reaction.And based on the lead compound"Diniconazole",a commercial triazole fungicide,novel 3-azolyl-quinoline derivatives were designed and synthesized using Friedlander reaction,on the assumption that introduce the chainlike-Diniconazole into heterocycles.Following are the synthetic routes. (?) (?)
6.The fungicidal activities against Penicilium digitatum of partial target compounds were tested, and initial screening show that the some compounds have activities against Penicilium digitatum.For example,compound 30n exhibited 90% inhibition activity against Penicilium digitatum in 50 ppm. Further fungicidal activity test found that the compound 30n still exhibited 99% inhibition activity against Septoria nodorum even in 10 ppm. (?)■
1.就最近几年来IMCR在杂环合成中的应用及aza-Wittig反应的最新进展进行了系统综述,并对三唑类杀菌剂和咪唑类杀菌剂进行了简单介绍。
2.应用连续的Passerini/Staudinger/aza-Wittig反应合成了4位酰氨基取代的4H-3,1-苯并噁嗪类化合物,对其反应规律、化合物性质进行了研究和讨论；对实验中丙酮酸的引入所产生的异常现象进行了解释,并通过膦亚胺与异氰酸酯的分子间aza-Wittig反应,经由碳二亚胺和分子内亲核加成,同样得到了4位酰氨基取代的4H-3,1-苯并噁嗪类化合物。为该类化合物的合成提供了新方法,该方法不仅原料易得,而且操作简单、条件温和、产率较高。合成路线如下：(?)
3.运用连续的Ugi/Staudinger/aza-Wittig反应来合成了3,4-二氢-2,3,4-三取代喹唑啉类化合物,并通过IR.1HNMR、13CNMR、MS和元素分析对目标化合物结构进行了表征,研究了其波谱性质。培养了其中一个代表性化合物的单晶,对该类化合物结构进一步进行确证和分析,通过对目标化合物分子结构的分析提出了可能的反应机理。这是第一例报道N,N-二取代的酰胺(无NH)可与碳二亚胺活性碳原子发生加成反应,反应过程中发生酰基重排而得到3,4-二氢喹唑啉衍生物,并对其中取代基对反应的影响进行了研究。合成路线如下：(?)
4.由异腈、羧酸、2-羰基苯胺和2-叠氮基苯甲醛出发,经连续的Ugi/Staudinger/aza- Wittig反应,得到了吲哚并[1,2-c]喹唑啉类化合物,采用IR、1HNMR、13CNMR、MS和元素分析等方法对目标化合物的结构进行了表征,讨论了其波谱性质。并通过其中一个代表性化合物的X-Ray单晶衍射分析,对该类化合物的结构进一步进行了确证。通过对目标化合物分子结构的分析提出了可能的反应机理,首次报道了Ugi反应产物中的次甲基碳对羰基的亲核加成得到吲哚化合物,讨论了取代基对反应的影响,并通过对照实验验证了其中喹唑啉环与吲哚环的形成是连续进行的。合成路线如下：(?)
5.将1,2,4-三唑环活性基团引入到Ugi反应产物的分子构架中,设计合成了新型的1,2,4-三唑化合物；并以烯唑醇为先导化合物,将烯唑醇链状化合物结构骨架设计到杂环分子中,应用Friedlander反应合成了新型3-唑基喹啉衍生物。具体路线如下：(?) (?)
6.在浓度为50 ppm时,对部分目标化合物进行了柑橘绿霉菌的抑菌活性测试,初步筛选结果表明部分化合物具有一定的抑制活性,如化合物30n对柑橘绿霉菌的抑制率达到90%。进一步活性测试发现,该化合物在10 ppm时,对小麦颖枯病仍然具有99%的防效。(?) 30n
Chemists have expressed great concern about N-heterocycles because of their good biological activities, such as broad-spectrum, efficient and low toxicity. The study of N-heterocycles chemistry have found a great deal of compounds with good prospects in pesticide、fungicide、herbicide、anti-Virus、anti-inflammatory and anti-tumor drugs. Some of them have been used as pesticide and medicine, the research on the synthesis and evaluate their biological activities of new N-heterocycle compounds is very active. In this dissertation we applied sequential IMCR/Staudinger/aza-Wittig reaction to design and synthesize 4-aminocarbonyl substituted 4H-3,1-benzoxazines,3,4-dihydro-2,3,4-trisubstitued quinazolines and indolo[1,2-c]quinazolines. And a series of unreported 1,2,4-triazole derivatives were designed and synthesized using Ugi reaction with the aim of evaluating their biological activities. Furthermore, novel 3-azolyl-quinoline derivatives were designed and synthesized using Friedlander reaction based on the lead compound "Diniconazole", a commercial triazole fungicide. The conditions of the syntheisis and the mechanism of the reaction were discussed, and the spectral properties of the target molecules were researched. The fungicidal activities of partial compounds were also tested. It may be summarized as follows:
1. The utilization of IMCR in the synthesis of heterocycles and the development of aza-Wittig reaction of recent years were reviewed, and a few commercial fungicides of triazole derivatives and imidazole derivatives were briefly introduced.
2.4-Aminocarbonyl substituted 4H-3,1-benzoxazine derivatives were synthesized using sequential Passerini/Staudinger/aza-Wittig reaction. The synthetic conditions and properties of the target compounds were studied and discussed. The unexpected phenomena of the reaction while pyruvic acid was used in the Passerini reaction were explained, and using further intermolecular aza-Wittig reaction via iminophosphoranes and isocyanates also give 4-aminocarbonyl substituted 4H-3,1-benzoxazine derivatives through carbodiimides and nucleophilic addition reaction. The synthetic routes could be used as new method to construct 4H-3,1-benzoxazines not only due to the easily accessible starting materials, but also for the simple operation, mild reaction conditions and the high yields. Following are the synthetic routes. (?) (?)
3.A series of 3,4-dihydro-2,3,4-trisubstitued quinazoline derivatives were synthesized using sequential Ugi/Staudinger/aza-Wittig reaction,and the structures of the target compounds were characterized via IR,1HNMR,13CNMR,MS and elemental analysis,and the spectral properties were also studied.Furthermore,the structure of the qninazoline derivatives was further confirmed and analysised through X-Ray single crystal diffraction by one representative compound.Through the structure analysis of the target molecules,a possible mechanism for the formation of the 3,4-dihydroquinazolines is proposed.It is the first report that N,N-disubstituted amides(containing no N-H moiety)could react with carbodiimides,and 3,4-dihydroquinazolines were formed through the further rearrangement of acyl group.The influence on the reaction of substituents was also studied, and following is the synthetic route. (?)
4.A sequential Ugi/Staudinger/aza-Wittig/nucleophilic addition reaction was developed to construct indolo[1,2-c]quinazoline derivatives,starting from carboxylic acid,2-azidobenzaldehyde, 2-acylaniline and isocyanide.And the structures of the compounds were characterized through IR, 1HNMR,13CNMR,MS and elemental analysis,the spectral properties were also discussed.The structure of the indolo[1,2-c]quinazoline derivatives was further established through X-Ray single crystal diffraction by one representative compound.Through the structure analysis of the target molecules,a possible mechanism for the formation of indolo[1,2-c]quinazolines is proposed.And this is the first report of the cyclization of the Ugi adduct to give indole ring system via the nucleophilic addition reaction of the methine group to the carbonyl group. Furthermore, the influence of substituents on the reaction was studied,and it is confirmed that the quinazoline ring together with the indole ring were formed sequentially through controlled reactions.Following is the synthetic route. (?)
5.A series of unreported 1,2,4-triazole derivatives were designed and synthesized using Ugi reaction.And based on the lead compound"Diniconazole",a commercial triazole fungicide,novel 3-azolyl-quinoline derivatives were designed and synthesized using Friedlander reaction,on the assumption that introduce the chainlike-Diniconazole into heterocycles.Following are the synthetic routes. (?) (?)
6.The fungicidal activities against Penicilium digitatum of partial target compounds were tested, and initial screening show that the some compounds have activities against Penicilium digitatum.For example,compound 30n exhibited 90% inhibition activity against Penicilium digitatum in 50 ppm. Further fungicidal activity test found that the compound 30n still exhibited 99% inhibition activity against Septoria nodorum even in 10 ppm. (?)■
引文
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