Efficient One-pot Synthesis of 1H-Pyrazolo[1,5-b]indazoles by a Domino Staudinger-Aza-Wittig Cyclization
作者:
Zhao, Fen-Fen;Yan, Yan-Mei;Zhang, Rui;Ding, Ming-Wu*
期刊:
SYNLETT ,2012年23(19):2850-2852 ISSN:0936-5214
通讯作者:
Ding, Ming-Wu
作者机构:
[Zhao, Fen-Fen; Yan, Yan-Mei; Ding, Ming-Wu] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Zhang, Rui] Wuhan Univ, Coll Chem & Mol Sci, Wuhan 430072, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
1H-pyrazolo[1,5-b]indazole;domino reaction;aza-Wittig reaction;azide;iminophosphorane
摘要:
1H-Pyrazolo[1,5-b]indazoles were prepared via a domino Staudinger–aza-Wittig cyclization in one-pot fashion, starting from easily accessible azides and triphenylphosphine.
语种:
英文
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2,3,5-三取代嘧啶-4(3H)-酮类化合物的合成新方法
作者:
钟莹;刘建超;王龙;丁明武
作者机构:
[钟莹; 刘建超; 王龙; 丁明武] 华中师范大学教育部农药与化学生物学重点实验室,湖北省武汉市珞喻路152号,430079
会议名称:
中国化学会第28届学术年会
会议时间:
2012-4-13
会议地点:
成都
会议主办单位:
中国化学会
会议论文集名称:
中国化学会第28届学术年会论文集
关键词:
氮杂Wittig反应;Baylis-Hillman反应;膦亚胺;嘧啶-4(3H)-酮
摘要:
<正>嘧啶酮是一类具有重要应用价值和良好生物活性的含氮杂环化合物,可用作抗肿瘤药物、止痛药物、杀菌剂、除草剂、杀虫剂等。我们曾利用三组分串联氮杂Wittig反应合成了一系列杂环并嘧啶酮结构的化合物[1,2],但该方法未被用于合成未稠合的嘧啶酮类化合物。这里我们报道从Baylis-Hillman反应产物出发,利
语种:
中文
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烯基膦亚胺的串联反应合成1,2,4,5-四取代咪唑
作者:
聂熠博;王龙;刘建超;丁明武
作者机构:
[聂熠博; 王龙; 刘建超; 丁明武] 华中师范大学教育部农药与化学生物学重点实验室,湖北省武汉市珞喻路152 号,430079
会议名称:
中国化学会第28届学术年会
会议时间:
2012-4-13
会议地点:
成都
会议主办单位:
中国化学会
会议论文集名称:
中国化学会第28届学术年会论文集
关键词:
氮杂Wittig反应;膦亚胺;咪唑
摘要:
<正>咪唑类化合物的合成方法有很多种,但是关于1,2,4,5-四取代咪唑的合成方法却少有报道。为了进一步拓展该类化合物合成和生物活性的研究,我们利用烯基膦亚胺的氮杂维悌希反应[1,2],提出了合成1,2,4,5-四取代咪唑的新方法。烯基膦亚胺1和异氰酸酯反应,产生中间体碳二亚胺2,2不经分离,直接和脂肪仲胺在碱性条件下反应,经连续的分子内Michael加成和异构化反应,生成1,2,4,5-四取代咪
语种:
中文
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Unexpected Synthesis of 2,4,5-Trisubstituted Oxazoles via a Tandem Aza-Wittig/Michael/Isomerization Reaction of Vinyliminophosphorane
作者:
Xie, Hai;Yuan, Ding;Ding, Ming-Wu*
期刊:
JOURNAL OF ORGANIC CHEMISTRY ,2012年77(6):2954-2958 ISSN:0022-3263
通讯作者:
Ding, Ming-Wu
作者机构:
[Xie, Hai; Ding, Ming-Wu; Yuan, Ding] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Xie, Hai] Shanxi Datong Univ, Coll Chem & Chem Engn, Datong 037009, Shanxi, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
摘要:
2,4,5-Trisubstituted oxazoles 6 were unexpectedly prepared from a tandem reaction of vinyliminophosphorane 3 with various acyl chlorides in a one-pot fashion.
语种:
英文
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Efficient Regioselective Synthesis of 3-Iodoindole N-Carboximidamides and N-Carboximidoates by a Sequential Aza-Wittig/Iodine Induced Cyclization
作者:
Nie Yibo;Duan Zhuan;Ding Mingwu*
期刊:
中国化学 ,2012年30(8):1807-1812 ISSN:1001-604X
通讯作者:
Ding Mingwu
作者机构:
[Ding Mingwu; Nie Yibo; Duan Zhuan] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Hubei, Peoples R China.
通讯机构:
[Ding Mingwu] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Hubei, Peoples R China.
关键词:
indole;aza-Wittig reaction;iodine;cyclization;iminophosphorane
摘要:
3-Iodoindole N-carboximidamides and N-carboximidoates 4 were prepared regioselectively via a sequential aza-Wittig/iodine induced cyclization, starting from easily accessible 2-alkynylphenyl iminophosphorane, isocyanates, various nucleophiles and iodine.
语种:
英文
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Temperature-dependent regioselective synthesis of 1,2,4-triazino[2,3-b] indazoles and 3H-1,4-benzodiazepines by domino-Staudinger/aza-Wittig/ isomerization reaction
作者:
Xie, Hai;Yu, Jian-Bo;Ding, Ming-Wu*
期刊:
European Journal of Organic Chemistry ,2011年2011(34):6933-6938 ISSN:1434-193X
通讯作者:
Ding, Ming-Wu
作者机构:
[Yu, Jian-Bo; Xie, Hai; Ding, Ming-Wu] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Xie, Hai] Shanxi Datong Univ, Coll Chem & Chem Engn, Datong 037009, Shanxi, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
Nitrogen heterocycles;Fused ring systems;Aza-Wittig reaction;Isomerization;Azides
摘要:
o-Azidobenzaldimine 8 reacted with triphenylphosphane at 0 °C with warming to room temperature to give 1,2,4-triazino[2,3-b]indazoles 12 by a domino-Staudinger/aza-Wittig/isomerization reaction. However, when heated to 80 °C the same reaction mixture afforded 3H-1,4-benzodiazepines 14 by a tandem-Staudinger/aza-Wittig reaction. © 2011 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
语种:
英文
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Facile Synthesis of 5-Carboxamide-oxazolines via a Passerini 3CC-Staudinger-aza-Wittig Sequence
作者:
Wu, Jing;Liu, Jian-Chao;Wang, Long;Ding, Ming-Wu*
期刊:
SYNLETT ,2011年2011(19):2880-2882 ISSN:0936-5214
通讯作者:
Ding, Ming-Wu
作者机构:
[Wu, Jing; Wang, Long; Liu, Jian-Chao; Ding, Ming-Wu] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
oxazoline;Passerini reaction;aza-Wittig reaction;Staudinger reaction;iminophosphorane
摘要:
5-Carboxamide-oxazolines were synthesized via a Passerini 3CC-Staudinger-aza-Wittig sequence in moderate to good yields, starting from easily accessible chloroacetaldehyde, isocyanides, and various acids. © Georg Thieme Verlag Stuttgart. New York.
语种:
英文
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Synthesis and Crystal Structure of 1-(4-Fluorophenyl)-2-hexylthiobenzo[4,5]-furo[3,2-d]-1,2,4-triazolo[1,5-a]pyrimidin-5(1H)-one
作者:
Hu Yang-Gen* ;Du Shi-Ming;Li Qing;Ding Ming-Wu
期刊:
Chinese Journal of Structural Chemistry ,2011年30(1):75-78 ISSN:0254-5861
通讯作者:
Hu Yang-Gen
作者机构:
[Hu Yang-Gen] Hubei Univ Med, Inst Med Chem, Shiyan 442000, Peoples R China.;[Hu Yang-Gen; Du Shi-Ming] Hubei Univ Med, Taihe Hosp, Dept Pharm, Shiyan 442000, Peoples R China.;[Li Qing] Hubei Univ Med, Dept Anesthesiol, Shiyan 442000, Peoples R China.;[Ding Ming-Wu] Cent China Normal Univ, Coll Chem, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Hu Yang-Gen] H;Hubei Univ Med, Inst Med Chem, Shiyan 442000, Peoples R China.
关键词:
synthesis;crystal structure,1-(4-fluorophenyl)-2-hexylthiobenzo[4,5]furo[3,2-d]-1,2,4-triazolo[1,5-a]pyrimidin-5(1H)-one
摘要:
The crystal structure of the title compound 1-(4-fluorophenyl)-2-hexylthio-benzo [4,5]furo[3,2-d]-1,2,4-triazolo[1,5-a]pyrimidin-5(1H)-one(C23H_21FN4O2S, Mr=436.5)has been prepared and determined by single-crystal X-ray diffraction. The crystal is of monoclinic, space group P21/n with a=13.9854(3),b=17.2678(4),c=18.1828(5)A,β=99.364(2)°,V=4332.58(18) A~ 3,Z=4, Dc=1.338,F(000)=1824,μ=0.185 mm~(-1), MoKa radiation(λ=0.71073),R=0.0538 and wR=0.1162 for 4728 observed reflections with I>2σ(I).X-ray diffraction analysis reveals the fused rings of benzo[4,5]furo[3,2-d]-1,2,4-triazolo[1,5-a]pyrimidin-5(1H)-one system are nearly coplanar. The crystal packing is mainly stabilized by weak intermolecular C-H…O hydrogen bond andπ-πinteractions
语种:
英文
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Efficient synthesis of thieno[2,3-d]pyrimidin-4(3H)-ones by a sequential aza-Wittig reaction/base catalyzed cyclization
作者:
Dai, Zhong-Xu;Chen, Hong* ;Liu, Ming-Guo;Ding, Ming-Wu
期刊:
HETEROCYCLIC COMMUNICATIONS ,2011年17(5-6):197-201 ISSN:0793-0283
通讯作者:
Chen, Hong
作者机构:
[Dai, Zhong-Xu; Liu, Ming-Guo; Chen, Hong] China Three Gorges Univ, Hubei Key Lab Nat Prod Res & Dev, Yichang 443002, Peoples R China.;[Ding, Ming-Wu] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Chen, Hong] C;China Three Gorges Univ, Hubei Key Lab Nat Prod Res & Dev, Yichang 443002, Peoples R China.
关键词:
aza-Wittig reaction;carbodiimide;iminophosphorane;thieno[2,3-d]pyrimidin-4(3H)-one
摘要:
7-Benzyl-5,6,7,8-tetrahydropyrido[4 ' ,3 ' :4,5]thieno[2,3-d] pyrimidin-4(3 H)-ones were synthesized by base catalyzed reactions of nucleophilic reagents (aliphatic amines, alcohols or phenols) with carbodiimides 4 , which in turn were obtained by the aza-Wittig reaction of iminophosphoranes 3 with aromatic isocyanates. 2011 · Copyright © by Walter de Gruyter.
语种:
英文
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New efficient synthesis of 2,3,4-trisubstituted 3,4-dihydroquinazolines by a Ugi 4CC/Staudinger/aza-Wittig sequence
作者:
Zhong, Ying;Wang, Long;Ding, Ming-Wu*
期刊:
Tetrahedron ,2011年67(20):3714-3723 ISSN:0040-4020
通讯作者:
Ding, Ming-Wu
作者机构:
[Wang, Long; Zhong, Ying; Ding, Ming-Wu] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
摘要:
A series of 2,3,4-trisubstituted 3,4-dihydroquinazoline 3 was prepared by intramolecular aza-Wittig reaction of amide carbonyl groups with methyldiphenyl iminophosphorane, which was obtained from a Ugi 4CC/Staudinger sequence. Further intramolecular Heck reaction of 3d'-g' in the presence of catalytic amount of Pd(OAc)(2) gave 6,12-dihydroindolo[2,1-b]quinazolines 4a-d in good yields. (C) 2011 Elsevier Ltd. All rights reserved.
语种:
英文
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Unexpected Synthesis of N-Acyl Indolines via a Consecutive Cyclization of Iminophosphorane
作者:
Li, Wen-Jing;Zhao, Fen-Fen;Ding, Ming-Wu*
期刊:
SYNLETT ,2011年2011(2):265-267 ISSN:0936-5214
通讯作者:
Ding, Ming-Wu
作者机构:
[Li, Wen-Jing; Zhao, Fen-Fen; Ding, Ming-Wu] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
N-acyl indoline;iminophosphorane;cyclization;Staudinger reaction
摘要:
N-Acyl indolines were obtained unexpectedly from a consecutive cyclization of iminophosphorane in refluxing xylene or 1,2-dichlorobenzene in good yields. This new approach provides an efficient and direct access to the biologically important indolines which are further oxidizable to indoles and oxindoles. © Georg Thieme Verlag Stuttgart.
语种:
英文
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CRYSTAL STRUCTURE OF 2-BUTYLAMINO-3-(4-FLUOROPHENYL) BENZOFURO[3,2-d]PYRIMIDIN-4(3H)-ONE
作者:
Hu, Ya-G* ;Chen, X-B;Gao, H-T;Ding, M-W
期刊:
Journal of Structural Chemistry ,2011年52(3):635-638 ISSN:0022-4766
通讯作者:
Hu, Ya-G
作者机构:
[Chen, X-B; Gao, H-T; Hu, Ya-G] Hubei Univ Med, Inst Med Chem, Shiyan 442000, Peoples R China.;[Ding, M-W] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[Hu, Ya-G] H;Hubei Univ Med, Inst Med Chem, Shiyan 442000, Peoples R China.
关键词:
crystal structure;benzo[4,5]furo[3,2-d]pyrimidin-4(3H)-one;aza-Wittig reaction
摘要:
The title compound (C20H18FN3O2, Mr = 351.37) is prepared and its crystal structure is determined by single crystal X-ray diffraction. The crystal is tetragonal, the P-42(1)c space group with a = 11.0922(6) Å, b = 11.0922(6) Å, c = 28.6271(15) Å, V = 3522.2(3) Å3, Z = 8, d
x
= 1.325 g/cm3, F(000) = 1472, μ = 0.095 mm−1, MoK
α radiation (λ = 0.71073), R = 0.0505, wR = 0.1090 for 2433 observed reflections with I > 2σ(I). The X-ray diffraction analysis reveals that all ring atoms in the benzo[4,5]furo[3,2-d]pyrimidinone moieties are almost coplanar.
语种:
英文
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Unexpected synthesis of indolo[1,2-c]quinazolines by a sequential Ugi 4CC-Staudinger-aza-Wittig-nucleophilic addition reaction
作者:
He, Ping;Nie, Yi-Bo;Wu, Jing;Ding, Ming-Wu*
期刊:
Organic & Biomolecular Chemistry ,2011年9(5):1429-1436 ISSN:1477-0520
通讯作者:
Ding, Ming-Wu
作者机构:
[Nie, Yi-Bo; Wu, Jing; Ding, Ming-Wu; He, Ping] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
摘要:
A new sequential Ugi-Staudinger-aza-Wittig-nucleophilic addition reaction was developed to construct indolo[1,2-c]quinazoline derivatives, starting from the easily accessible 2-azidobenzaldehyde, carboxylic acid, 2-acylaniline and isocyanide. It is noteworthy that this is the first report of the cyclization of the Ugi adduct to give a dihydroindole ring system with two quaternary carbon centers, via the nucleophilic addition reaction of the methine group to the carbonyl group. ©The Royal Society of Chemistry 2011.
语种:
英文
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噁唑衍生物的合成新方法
作者:
解海;赵芬芬;丁明武
作者机构:
[解海; 赵芬芬; 丁明武] 华中师范大学教育部农药与化学生物学重点实验室
会议名称:
有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会
会议时间:
2010-10-18
会议地点:
中国重庆
会议论文集名称:
有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会论文摘要集
关键词:
噁唑;杂环;氮杂维悌希反应
摘要:
<正>噁唑衍生物在天然产物、药物化学和材料化学领域应用广泛.由于天然存在的噁唑类化合物结构的多样性和复杂性,寻求温和、简单和有效地合成噁唑类化合物一直受到有机合成工作者的高度重视.文献中已报道了多种合成噁唑类化合物的方法,包括分子内氮杂Wittig反应方法.我们曾经利用氮杂Wittig反应合成了5-烷氧基噁唑类化合物.这里进一步报道一条应用分子内氮杂Wittig异构芳香化反应来合成2,4,5-三取
语种:
中文
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1,2,4-三取代咪唑的合成新方法
作者:
聂熠博;刘帅;丁明武
作者机构:
[聂熠博; 刘帅; 丁明武] 华中师范大学教育部农药与化学生物学重点实验室
会议名称:
有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会
会议时间:
2010-10-18
会议地点:
中国重庆
关键词:
咪唑;杂环;氮杂维悌希反应
摘要:
<正>咪唑类化合物是一类有着良好生物活性和药理活性的含氮杂环,在医药、农药、高性能复合材料、染料和金属防腐等诸多领域显示了独特性能.合成咪唑类化合物有多种方法,但通过氮杂wittig反应合成1,2,4-三取代咪唑的报道并不多见.氮杂Wittig反应由于具有反应条件温和,副反应少,且反应多通过串联进行,操作简便,总收率高等特点,现已成为一种合成新型氮杂环及生物活性的天然杂环有机化合
语种:
中文
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Synthesis and biological activities of enantioriched 1 -Aryl-2-(1H-1,2,4- triazol-1-yl)ethanols
作者:
Xu Shengzhen* ;Ming Zhihui;Yang Jiaoyan;Yang Shao;Ding Mingwu;...
期刊:
有机化学 ,2010年30(2):285-288 ISSN:0253-2786
通讯作者:
Xu Shengzhen
作者机构:
[Xu Shengzhen; Ding Mingwu; Ming Zhihui; Xiao Wenjing] Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.;[Yang Shao; Yang Jiaoyan] Cent China Normal Univ, Coll Life Sci, Wuhan 430079, Peoples R China.
通讯机构:
[Xu Shengzhen] C;Cent China Normal Univ, Minist Educ, Key Lab Pesticide & Chem Biol, Wuhan 430079, Peoples R China.
关键词:
***;手性;14α-脱甲基化酶;抑菌活性
摘要:
取代苯乙烯1与KHSO_5在手性催化剂2存在的条件下反应,生成1-芳基环氧化物3,3与1H-1,2,4.***在固体碳酸钾催化下作用,得到手性的1-芳基-2-(1H-1,2,4-***-1-基)乙醇衍生物4.部分4对甾醇14α-脱甲基化酶表现出强结合作用.
语种:
中文
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New efficient synthesis of pyrimido[1,6-c]quinazolin-4-ones by a Biginelli 3CC/Staudinger/aza-Wittig sequence
作者:
Li, Wen-Jing;Liu, Shuai;He, Ping;Ding, Ming-Wu*
期刊:
Tetrahedron Letters ,2010年66(41):8151-8159 ISSN:0040-4039
通讯作者:
Ding, Ming-Wu
作者机构:
[Li, Wen-Jing; Liu, Shuai; Ding, Ming-Wu; He, Ping] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
通讯机构:
[Ding, Ming-Wu] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Peoples R China.
摘要:
Dihydropyrimidinone azides 1, obtained from trimethylsilyl chloride-catalyzed Biginelli reaction of 2-azidobenzaldehyde, ethyl acetoacetate, and urea (or thiourea) at room temperature, reacted with triphenylphosphine to give iminophosphorane 2. A tandem aza-Wittig reaction of iminophosphorane 2 with isocyanate, acyl chloride or CS2 in the presence of K2CO3 or NEt3 generated pyrimido[1,6-c]quinazolin-4-ones 4, 6 or 8 in moderate to good yield.
语种:
英文
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2,2'-二取代双[3-芳基喹唑啉-4(3H)-酮]的合成
作者:
Yang Xuhong* ;Wu Minghu;Ding Mingwu
期刊:
有机化学 ,2010年30(7):1032-1038 ISSN:0253-2786
通讯作者:
Yang Xuhong
作者机构:
[Yang Xuhong; Wu Minghu] Xianning Coll, Fac Chem & Life Sci, Xianning 437100, Peoples R China.;[Ding Mingwu] Cent China Normal Univ, Key Lab Pesticide & Biol, Minist Educ, Wuhan 430071, Peoples R China.
通讯机构:
[Yang Xuhong] X;Xianning Coll, Fac Chem & Life Sci, Xianning 437100, Peoples R China.
关键词:
喹唑啉-4(3H)-酮;膦亚胺;碳二亚胺;二酚;氮杂Wittig反应;合成
摘要:
研究了多米诺骨牌反应合成2,2'-二取代双[3-芳基喹唑啉-4(3H)-酮]衍生物的方法.该方法应用膦亚胺1与芳基异氰酸酯的氮杂Wittig反应得到碳二亚胺2,接着与二酚在碳酸钾存在下反应,合成了28个未见文献报道的双喹唑啉酮衍生物4.所得产物4的结构经IR,~1H NMR,MS和元素分析测定,并且采用X射线衍射分析方法进一步确证了化合物 4z的结构
语种:
中文
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Efficient synthesis and biological evaluation of some 2,4-diamino-furo[2,3-d]pyrimidine derivatives
作者:
Hu, Yang-Gen* ;Wang, Yan;Du, Shi-Ming;Chen, Xiao-Bao;Ding, Ming-Wu
期刊:
Bioorganic & Medicinal Chemistry Letters ,2010年20(21):6188-6190 ISSN:0960-894X
通讯作者:
Hu, Yang-Gen
作者机构:
[Hu, Yang-Gen; Chen, Xiao-Bao] Hubei Med Univ, Inst Med Chem, Shiyan 442000, Peoples R China.;[Wang, Yan] Hubei Med Univ, Inst Basic Med Sci, Shiyan 442000, Peoples R China.;[Hu, Yang-Gen; Du, Shi-Ming] Hubei Med Univ, Taihe Hosp, Dept Pharm, Shiyan 442000, Peoples R China.;[Ding, Ming-Wu] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Coll Chem, Wuhan 430079, Peoples R China.
通讯机构:
[Hu, Yang-Gen] H;Hubei Med Univ, Inst Med Chem, Shiyan 442000, Peoples R China.
关键词:
Antitumor activity;Aza-Wittig reactions;Ethyl 4-alkylamino-2-arylamino-6-methyl-furo[2,3-d]pyrimidine-5- carboxylate
摘要:
The carbodiimides 2, obtained from aza-Wittig reactions of iminophosphorane 1 with aromatic isocyanates, reacted with ammonia to give ethyl 3,4-dihydro-6-methyl-4-oxo-2-arylamino-furo[2,3-d]pyrimidine-5-carboxylate 3. Further reaction of 3 with POCl3 and various amines generated ethyl 4-alkylamino-2-arylamino-6-methyl-furo[2,3-d]pyrimidine-5-carboxylate 5 in good yields. Their structures were confirmed by 1H NMR, EI-Ms, IR and elemental analysis. Compound 5b was further analyzed by single crystal X-ray diffraction. Compound 5 exhibited cytotoxicity against two lung cancer cell lines. For example, compound 5a showed the best inhibition activities against A459 with IC50 0.8 μM. © 2010 Elsevier Ltd. All rights reserved.
语种:
英文
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Efficient Synthesis of New Tetracyclic Benzofuro[3,2-d]-imidazo[1,2-a] pyrimidine-2,5-(1 H,3 H)-diones
作者:
Hu Yanggen;Liu Min;Ding Mingwu*
期刊:
中国化学 ,2010年28(2):309-312 ISSN:1001-604X
通讯作者:
Ding Mingwu
作者机构:
[Ding Mingwu; Liu Min; Hu Yanggen] Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Hubei, Peoples R China.;[Hu Yanggen] Yunyang Med Coll, Taihe Hosp, Dept Pharm, Shiyan 442000, Hubei, Peoples R China.;[Hu Yanggen] Yunyang Med Coll, Inst Med Chem, Shiyan 442000, Hubei, Peoples R China.
通讯机构:
[Ding Mingwu] C;Cent China Normal Univ, Key Lab Pesticide & Chem Biol, Minist Educ, Wuhan 430079, Hubei, Peoples R China.
关键词:
benzofuro[3,2-d]imidazo[1,2-a]pyrimidine-2,5-(1H,3H)-dione;iminophosphorane;aza-Wittig reaction;isocyanate;carbodiimide
摘要:
The aza-Wittig reaction of iminophosphorane (1) with aromaic isocyanates gave carbodiimides (2), which were allowed to react further with α-amino ester in the presence of a catalytic amount of sodium ethoxide to give selectively new tetracyclic benzofuro[3,2-d]imidazo[1,2-a]pyrimidine-2,5-(1H,3H)-diones (5) in good yields. X-ray structure analysis of 5i verified the proposed structure and the reaction selectivity. © 2010 SIOC, CAS, Shanghai, & WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
语种:
英文
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