A química medicinal na próxima década

Montanari, Carlos Alberto

doi:10.1590/s0100-40422000000100024

Cited by 9 publications

(7 citation statements)

References 13 publications

(14 reference statements)

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“…Portanto, não se trata de uma busca exaustiva. Apenas por brevidade inerente, as palavras escolhidas foram: QUÍMICA MEDICINAL [13][14][15][16][17][18][19][20][21][22] , QSAR 14, 23-62 e PLANEJAMENTO DE FÁRMACOS 14,18,21,44,45,56,57,59,[63][64][65][66][67][68][69][70][71][72][73][74][75][76][77][78][79] .…”

Section: Cenário Científico E Tecnológico No País Depois De 1991unclassified

Química Medicinal: 25 anos de planejamento racional de fármacos

2002

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is commemorating its 25 th anniversary, and this paper is intended to draw an overview of the Brazilian Medicinal Chemistry over all these years. In 1977 Brazil had almost no activities at all in the field, albeit many efforts were already on the way for encouraging Brazilian Scientists to enter the area. Among many different endeavours to help medicinal chemists to fulfil their proposals and the establishment of an ongoing research with the help of networks, the Sociedade Brasileira de Química created, in 1991, its own Division on Structure and Activity Relationship, which became the Division of Medicinal Chemistry, in 1997.

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Section: Cenário Científico E Tecnológico No País Depois De 1991unclassified

Química Medicinal: 25 anos de planejamento racional de fármacos

2002

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“…O Químico Medicinal, por ex., que freqüentemente trabalha com compostos homólogos, pode utilizar-se da determinação dos deslocamentos químicos tanto como uma variável para estudos da Relação Quantitativa Estrutura-Atividade (QSAR) [4][5][6] , quanto como "insight" para definir restrições estruturais a serem utilizadas em cálculos teóricos que, por sua vez, visam também fornecer outros parâmetros para estudos QSAR.…”

Section: Introductionunclassified

Aplicação de análise de componentes principais para verificação de atribuições de sinais nos espetros de RMN ¹H: o caso dos 3-aril (1,2,4)-oxadiazol-5-carboidrazida benzilidenos

Silva¹,

Malvestiti²,

Hallwass³

et al. 2005

Quím. Nova

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“…Similar treatment of o-(trimethylsilyl)phenyliodonium triflate 1 with Bu 4 NF in the presence of nitrones 4 afforded the corresponding benzisoxazolines (5) in high yields, respectively. Similar treatment of o-(trimethylsilyl)phenyliodonium triflate 1 with Bu 4 NF in the presence of nitrones 4 afforded the corresponding benzisoxazolines (5) in high yields, respectively.…”

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A Convenient and Efficient Synthesis of Benzotriazoles and Benzisoxazolines Using Anew Hypervalent Iodine-Benzyne Precursor

Kitamura¹,

Todaka²,

Shin-machi³

et al. 1998

Heterocyclic Communications

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Reaction of (phenyl) [o-(trimethylsilyl)phenyl]iodonium triflate with organic azides and nitrones using Bu 4 NF gave benzotriazoles and benzisoxazolines in high yields, respectively. This reaction indicates that benzyne is generated under mild conditions and efficiently trapped with the 1,3-dipoles to give heterocyclic compounds.Recently much attention has been paid to the use of hypervalent iodine compounds in organic synthesis (1-7). Previously we have found that (phenyl)[o-(trimethylsilyl)phenyl]iodonium triflate (1) acts as an excellent benzyne precursor and generates benzyne quantitatively by a simple treatment of o-(trimethylsilyl)phenyliodonium triflate 1 with Bu 4 NF under very mild conditions as shown in Scheme 1 (8).The merits of the use of the hypervalent iodine-benzyne precursor 1 includes (a) the stability of the precursor 1, (b) no requirement of a strong base or high temperature, and (c) the quantitative generation of benzyne under mild conditions.If the hypervalent iodine-benzyne precursor 1 can be applied to the reactions with 1,3-dipoles such as azides and nitrones, the reaction of 1 will provides a useful methodology for synthesis of heterocyclic skeletons.In this paper, we report an efficient and convenient synthesis of benzotriazoles and benzisoxazolines by means of the hypervalent iodine-benzyne precursor 1. 1 100% Scheme 1. 205 Brought to you by | Purdue University Libraries Reaction of o-(trimethylsilyl)phenyliodonium triflate 1 with aryl azides (2a-d) could be conducted in CH 2 CI 2 simply by adding Bu 4 NF. A solution of 1 and aryl azides in CH 2 CI 2 was treated with aTHF solution ofBu 4 NF at 0 °C and the reaction mixture was stirred at room temperature for 20 min. Separation by column chromatography on silica gel gave 1-arylbenzotriazoles (3a-d) in high yields. The results are given in Table 1.This reaction was applied to ethyl 2-azidopropionate (2 e)and 2-azido-1-octadecene (21), which reacted with benzyne generated from 1 to yield the corresponding benzotriazoles (3 e and f). As shown in Table 1, o-(trimethylsilyl)phenyliodonium triflate 1 is a useful reagent for benzotriazole synthesis. Even in the reaction of athermally unstable vinyl azide or an azide bearing functional ester group, 1 acts as the benzyne precursor and undergoes the 1,3-dipolar cycloaddition efficiently.Abstract: New synthetic routes for antimicrobial mesoionics 4-methyl-1.3.4-thiadiazolium-2-aminide and 4-aryl-1.3.4thiadiazolium-2-aminide and their precursors are reported. Through the reported procedure, antimicrobial 1,4-diaroylthiosemicarbazides can be obtained in high purity degree.

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A química medicinal na próxima década

Cited by 9 publications

References 13 publications

Química Medicinal: 25 anos de planejamento racional de fármacos

Química Medicinal: 25 anos de planejamento racional de fármacos

Aplicação de análise de componentes principais para verificação de atribuições de sinais nos espetros de RMN ¹H: o caso dos 3-aril (1,2,4)-oxadiazol-5-carboidrazida benzilidenos

A Convenient and Efficient Synthesis of Benzotriazoles and Benzisoxazolines Using Anew Hypervalent Iodine-Benzyne Precursor

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