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Bhalay, Gurdip; Cowell, Daniel D.; Hone, Neal D.; Scobie, Martin; Baxter, Anthony D.

doi:10.1023/a:1009612923900

Cited by 15 publications

(5 citation statements)

References 2 publications

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“…Other small molecule mixture-based libraries include: (1) the synthesis of 4-thiazolidinones and 4-metathiazanones derived from three-component condensation of an amino acid ester or a resin-bound amino acid, an aldehyde, and an α-mercaptocarboxylic acid (the identification of cyclooxygenase-1 inhibitors from 4-thiazolidinone combinatorial libraries has recently been reported by Look and co-workers); (2) the synthesis of hydantoin and thiohydantoin libraries through isocyanate and thioisocyanate formation on the solid support and intramolecular cyclization; (3) the synthesis of amide-based small molecules using various cyclic/acyclic amines, primary/secondary amines, and different protected bifunctional amines as nucleophiles to react with different anhydrides; (4) the synthesis of phosphoramidate combinatorial libraries from oxidation with primary and secondary amines to support-bound aminodiol scaffolds; (5) the synthesis of dihydropyridines, pyridines, and pyrido[2,3- d ]pyrimidines; and (6) the synthesis of a library composed of 1 296 N-acylated dipeptides with the identification of inhibitors of phosphomannose isomerase having low micromolar activity …”

Section: Existing Mixture-based Heterocyclic and Small Organic Molecu...mentioning

confidence: 99%

Mixture-Based Synthetic Combinatorial Libraries

et al. 1999

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Section: Existing Mixture-based Heterocyclic and Small Organic Molecu...mentioning

confidence: 99%

Mixture-Based Synthetic Combinatorial Libraries

et al. 1999

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“…Because many more libraries are published annually without associated biological data and are of equal interest to the combinatorial and medicinal chemical communities, a compilation of these types of constructs is included in this review. In 1998, there were 247 libraries of this genus. − …”

mentioning

confidence: 99%

Comprehensive Survey of Combinatorial Library Synthesis: 1998

Dolle¹,

Nelson²

1999

J. Comb. Chem.

286

133

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An exhaustive compilation of biologically active libraries covering the years 1992-1997 was presented in a previous review [1a]. In that review, libraries were divided among 4 major categories, including those active against proteases, non-proteolytic enzymes, Gprotein coupled receptors, and non-G-protein coupled receptors. A generic structure for each library was provided as well as the structure of the most active member. The number of biologically active libraries reported in the literature during this time period (86 total) represents <25% of the total number of published library constructs. Disclosure of library synthesis without accompanying screening data is a more common occurrence. Because these types of libraries are equally important to the practicing combinatorial chemist, it was thought that a comprehensive listing of such libraries spanning the years 1992-1997 would be a useful supplement to the previous review [1a,b].Library constructs [2-248] listed herein are relegated to one of five tables. Table 1 is entitled 'Scaffold derivatization' and includes all constructs in which a multi-functional scaffold is modified in some fashion to create a library. An example of a construct found in Table 1 would be the sequential addition of three nucleophiles to trichloropyrimidine. Table 2, entitled 'Acyclic synthesis', lists all linear constructs such as those derived from multi-component Ugi condensations.

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“…Using different amino acids (first site of diversity-R 1 ) and different alkyl groups (second site of diversity-R 2 ), this method allowed preparation of a broad range of new hydantoin derivatives. Instead of triphosgene, diphosgene was also applied in solid-phase hydantoin synthesis [131]. Hydantoins can be obtained by the application of the Hofmann degradation reaction (Hofmann rearrangement) of malonamides [132,133].…”

Section: Comparison With Other Methods Affording Hydantoinsmentioning

confidence: 99%

The Bucherer–Bergs Multicomponent Synthesis of Hydantoins—Excellence in Simplicity

et al. 2021

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Hydantoins and their hybrids with other molecules represent a very important group of heterocycles because they exhibit diverse biological and pharmacological activities in medicinal and agrochemical applications. They also serve as key precursors in the chemical or enzymatic synthesis of significant nonnatural α-amino acids and their conjugates with medical potential. This review provides a comprehensive treatment of the synthesis of hydantoins via the Bucherer–Bergs reaction including the Hoyer modification but limited to free carbonyl compounds or carbonyl compounds protected as acetals (ketals) and cyanohydrins used as starting reaction components. In this respect, the Bucherer–Bergs reaction provides an efficient and simple method in the synthesis of important natural products as well as for the preparation of new organic compounds applicable as potential therapeutics. The scope and limitations, as well as a comparison with some other methods for preparing hydantoins, are also discussed.

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Untitled

Cited by 15 publications

References 2 publications

Mixture-Based Synthetic Combinatorial Libraries

Mixture-Based Synthetic Combinatorial Libraries

Comprehensive Survey of Combinatorial Library Synthesis: 1998

The Bucherer–Bergs Multicomponent Synthesis of Hydantoins—Excellence in Simplicity

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