Chemistry strategies in early drug discovery: an overview of recent trends

Colombo, Matteo; Peretto, Ilaria

doi:10.1016/j.drudis.2008.03.007

Cited by 169 publications

(61 citation statements)

References 56 publications

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“…There is, meanwhile, a consensus that micro reactors and continuous fl ow are powerful tools for various applications for the discovery and development process in research laboratories within the pharmaceutical, agro, fi ne-chemical, petrochemical and fragrance industries [3,31] . This is, for example, demonstrated by giving continuous processing Top-1 priority in the 10 Green Engineering prime measures stated by the multi-industrial American Chemical Society ' s Green Chemistry Institute Pharmaceutical Roundtable [32] .…”

Section: Micro Reaction Technology For Use In Pharmacy and Its Procesmentioning

confidence: 99%

“…Continuous fl ow reactors for drug discovery have been reported as a tool used in pharmaceutical companies to increase the numbers of compounds synthesized and evaluate biological activity faster [3,8,9] , as well as use in industrial production [10,11] . Many more reviews followed, and increasingly specialized either on chemistry [12] , chemical engineering [13] or devices [14] .…”

Section: Micro Reaction Technology: Chemistry In Fl Owmentioning

confidence: 99%

“…Chemists are searching for ways to simplify, improve and automate synthetic protocols, for example, by the use of polymer-assisted solution-phase synthesis, microwave-assisted organic synthesis [1,2] , micro reactors, fl ow chemistry [3,4] and green chemistry [5] .…”

Section: Micro Reaction Technology: Chemistry In Fl Owmentioning

confidence: 99%

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Micro reactor and flow chemistry for industrial applications in drug discovery and development

Baraldi¹,

Hessel

2012

Green Processing and Synthesis

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In this review, case studies focused on syntheses of active pharmaceutical ingredients, intermediates and lead compounds are reported employing micro reactors and continuous fl ow technology in areas such as medicinal chemistry, chemical development and manufacturing. The advantages of fl ow technology are currently very clear as opposed to conventional batch methods. Most strikingly and relevant for pharmaceutical ' s time-to-market needs, fl ow processing has the important advantage of the ease with which reaction conditions can be scaled. As this technology is new and has major full-process scale implications, we also wanted to point out that this cannot be applied and released to all chemistries yet, thereby also critically mirroring disadvantages and advantages of the step-change technology. However, the positive impact has been dominating and thus pharmaceutical and fi ne-chemical industries have increased their awareness and interest in fl ow chemistry applications. Beyond pharmaceutical syntheses, this review aims to conclude with the special needs of pharmacy on fl ow and micro reactor chemistry, which is not the same as for the fi ne-chemical industry. Here, the needs of Brazil are considered, as the mirroring of micro reactor and fl ow chemistry was done from a European -academic and business -perspective. The hope is to stimulate and promote fl ow developments in emerging developing nations.

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Section: Micro Reaction Technology For Use In Pharmacy and Its Procesmentioning

confidence: 99%

Section: Micro Reaction Technology: Chemistry In Fl Owmentioning

confidence: 99%

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Micro reactor and flow chemistry for industrial applications in drug discovery and development

Baraldi¹,

Hessel

2012

Green Processing and Synthesis

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“…The rational design of the pharmaceutical form should, however, start with the characterization of the active pharmaceutical ingredients (APIs) in question, in order to improve the quality parameters of the pharmaceutical products. The process involving the research and development of new drugs has increased markedly, and there is a great need for the development of new pharmacologically active compounds that are effective against different pathologies even without treatment, which can replace those existing and reduce costs as well as any side effects [1].…”

Section: Introductionmentioning

confidence: 99%

Thermal characterization of some guanylhydrazones by thermal and nonthermal techniques

galvão

Brito

Dantas

et al. 2014

J Therm Anal Calorim

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2-[(3,5-di-tert-butyl-4-hydroxyphenyl)methylene]-hydrazinecarboximidamide (WE010), 2-([1,1 0 -biphenyl]-4-ylmethylene)-hydrazinecarboximidamide (WE014), and 2-[(3,4-dichlorophenyl)methylene]-hydrazinecarboximidamide (WE017) are guanylhydrazone derivatives widely studied biologically and chemically; however, there are no studies regarding their thermal behaviors. The present study aims to apply the thermal analyses: differential scanning calorimetry (DSC), differential scanning calorimetry coupled to the photovisual system (DSC-photovisual), and thermogravimetry (TG), to characterize the guanylhydrazones, as well as HPLC and FTIR. The DSC curve of WE010 shows a melting process with T onset at 190°C and peak at 193.5°C (DH 41.0 J g -1 ). Due to the symmetry of the melting peaks obtained by DSC, it is possible to calculate the purity of the sample (98.87 %). The DSC curve of WE014 shows the melting process in the range of 208-213°C, with a melting peak at 211°C (DH 61 J g -1 ).The DSC curve of WE017 showed T onset at 215°C and peak temperature of 219°C (DH 55 J g -1 ). The TG curve of WE010, WE014, and WE017 presents initial decomposition temperatures of 186.95, 197.31, and 195.44°C, respectively. The DSC-photovisual confirmed the results of DSC and TG. The HPLC determined the purities of the samples and confirmed the results of DSC. The FTIR confirmed the thermal data. Thus, the use of thermal analysis is an important tool for the characterization of molecules with therapeutic potential contributing to the characterization and evaluation of their stability as well as nonthermal technique with complementary tool.

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“…This technique has several advantages over classical stepby-step synthetic routes (linear or convergent) not only from atom-economy and eco-friendly perspective but also by the operational simplicity of these procedures that offer a variety of carbon-hetero atom bonds formation [60,61]. Furthermore, this technique provides highest speed reaction and rapid increase in reaction temperature; it is specific and does not require contact between the power source and the reaction vessel [62].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of New (E)-2-(1H-Indole-3-ylcarbonyl)-3-heteroaryl-acrylonitriles via Microwave-Assisted Knoevenagel Condensation

Treuer

De-la-Torre

Gutiérrez

2017

Journal of Chemistry

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Given the broad spectrum of biological uses of heteroaryl-acrylonitrile derivatives, it is necessary to find simple methods to synthesize and diversify this family of compounds. We report a stereoselective synthesis of a series of new (E)-2-(1H-indole-3-ylcarbonyl)-3-heteroaryl-acrylonitriles ( a-i) obtained from 3-(cyanoacetyl)indole and heteroaryl-aldehydes under microwaveassisted Knoevenagel reaction at 300 W of potency and 100 ∘ C. The desired derivatives ( a-i) were obtained with variable yields (30-94%) and time reactions (8-90 min). All the heteroaryl-acrylonitriles were characterized by physicoanalytical techniques such IR, 1 H, 13 C NMR, and electrospray mass spectrometry.

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Chemistry strategies in early drug discovery: an overview of recent trends

Cited by 169 publications

References 56 publications

Micro reactor and flow chemistry for industrial applications in drug discovery and development

Micro reactor and flow chemistry for industrial applications in drug discovery and development

Thermal characterization of some guanylhydrazones by thermal and nonthermal techniques

Synthesis of New (E)-2-(1H-Indole-3-ylcarbonyl)-3-heteroaryl-acrylonitriles via Microwave-Assisted Knoevenagel Condensation

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