α‐Amino Acid‐Isosteric α‐Amino Tetrazoles

Zhao, Ting; Kurpiewska, Katarzyna; Kalinowska‐Tłuścik, Justyna; Herdtweck, Eberhardt; Dömling, Alexander

doi:10.1002/chem.201504520

Cited by 35 publications

(20 citation statements)

References 44 publications

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“…Experts from all essential areas of early DD—industry, academia, and SMEs—now jointly produce high-quality output for the wider public benefit. In this time, the PPP has published >30 articles and the results from the first crowdsourced ideas gradually disseminate in the public domain for everyone to assess (6, 12, 13, 15, 19–48). …”

Section: Resultsmentioning

confidence: 99%

The European Lead Factory: A Blueprint for Public–Private Partnerships in Early Drug Discovery

Karawajczyk¹,

Orrling

Vlieger

et al. 2017

Front. Med.

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The European Lead Factory (ELF) is a public–private partnership (PPP) that provides researchers in Europe with a unique platform for translation of innovative biology and chemistry into high-quality starting points for drug discovery. It combines an exceptional collection of small molecules, high-throughput screening (HTS) infrastructure, and hit follow-up capabilities to advance research projects from both private companies and publicly funded researchers. By active interactions with the wider European life science community, ELF connects and unites bright ideas, talent, and experience from several disciplines. As a result, ELF is a unique, collaborative lead generation engine that has so far resulted in >4,500 hit compounds with a defined biological activity from 83 successfully completed HTS and hit evaluation campaigns. The PPP has also produced more than 120,000 novel innovative library compounds that complement the 327,000 compounds contributed by the participating pharmaceutical companies. Intrinsic to its setup, ELF enables breakthroughs in areas with unmet medical and societal needs, where no individual entity would be able to create a comparable impact in such a short time.

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Section: Resultsmentioning

confidence: 99%

The European Lead Factory: A Blueprint for Public–Private Partnerships in Early Drug Discovery

Karawajczyk¹,

Orrling

Vlieger

et al. 2017

Front. Med.

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“…[82] The synthesis of the cysteine analogue could not be achieved by use of mercaptoacetaldehyde dimer, the desired Ugi product being not formed; therefore, a different strategy was devised. [82] The synthesis of the cysteine analogue could not be achieved by use of mercaptoacetaldehyde dimer, the desired Ugi product being not formed; therefore, a different strategy was devised.…”

Section: Synthesis Of 13-thiazoles and Thiazolidinesmentioning

confidence: 99%

1,4‐Dithiane‐2,5‐diol: An Attractive Platform for the Synthesis of Sulfur‐Containing Functionalized Heterocycles

2018

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This microreview highlights the utility of 1,4‐dithiane‐2,5‐diol (1) as a source for the in situ generation of 2‐mercaptoacetaldehyde (2), a versatile two‐carbon synthon featuring both electrophilic and nucleophilic reaction centres and widely utilized as an attractive platform for the preparation of sulfur‐containing molecules. We discuss the chemistry involved, mainly focusing on its applications to the construction of sulfur‐containing heterocyclic compounds including the thiophene and 1,3‐thiazole families and other different sulfur–nitrogen and sulfur–oxygen heterocycles that continue to be a pillar of organic synthesis as a result of their broad application in organic and medicinal chemistry.

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“…The unique application of the Asinger 4-CR/azido-Ugi 3-CR combination was reported by Domling and co-workers, 6 while, quite recently, the first example of diastereoselective azido-Ugi reaction was reported by Nenajdenko and co-workers, 7 employing secondary amines. Summing, at the best of our knowledge, no examples of diastereoselective multicomponent transformations have been reported until now on thiazoline substrates.…”

Section: ■ Introductionmentioning

confidence: 95%

Sequential Multicomponent Strategy for the Diastereoselective Synthesis of Densely Functionalized Spirooxindole-Fused Thiazolidines

et al. 2018

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We developed two Ugi-type three-component reactions of spirooxindole-fused 3-thiazolines, isocyanides, and either carboxylic acids or trimethylsilyl azide, to give highly functionalized spirooxindole-fused thiazolidines. Two diverse libraries were generated using practical and robust procedures affording the products in typically good yields. The obtained thiazolidines proved to be suitable substrates for further transformations. Notably, both the Ugi-Joullié and the azido-Ugi reactions resulted highly diastereoselective, affording predominantly the trans-configured products, as confirmed by X-ray crystallographic analysis.

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α‐Amino Acid‐Isosteric α‐Amino Tetrazoles

Cited by 35 publications

References 44 publications

The European Lead Factory: A Blueprint for Public–Private Partnerships in Early Drug Discovery

The European Lead Factory: A Blueprint for Public–Private Partnerships in Early Drug Discovery

1,4‐Dithiane‐2,5‐diol: An Attractive Platform for the Synthesis of Sulfur‐Containing Functionalized Heterocycles

Sequential Multicomponent Strategy for the Diastereoselective Synthesis of Densely Functionalized Spirooxindole-Fused Thiazolidines

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