1581682-03-2Relevant academic research and scientific papers
Bicyclo[1.1.1]pentane-Derived Building Blocks for Click Chemistry
Kokhan, Serhii O.,Valter, Yevheniia B.,Tymtsunik, Andriy V.,Komarov, Igor V.,Grygorenko, Oleksandr O.
, p. 6450 - 6456 (2017)
Syntheses of bicyclo[1.1.1]pentane-derived azides and terminal alkynes – interesting substrates for click reactions – are described. With a few exceptions, these compounds were prepared in two or three steps starting from common synthetic intermediates – the corresponding carboxylic acids. The key step in the synthesis of 1-azidobicyclo[1.1.1]pentanes is a copper-catalysed diazo-transfer reaction with imidazole-1-sulfonyl azide. The preparation of bicyclo[1.1.1]pentyl-substituted alkynes relies on a Seyferth–Gilbert homologation with dimethyl 1-diazo-2-oxopropylphosphonate (Ohira–Bestmann reagent). Both types of target compounds were found to be suitable substrates for click reactions, and thus they are promising building blocks for medicinal, combinatorial and bioconjugate chemistry. A practically important side result of this study was a multigram preparation of Boc-monoprotected 1,3-diaminobicyclo[1.1.1]pentane – a representative bicyclic conformationally restricted diamine derivative.
SOLID FORMS OF A COT INHIBITOR COMPOUND
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Paragraph 0239, (2021/10/11)
Disclosed are solid forms of a Cot (cancer Osaka thyroid) inhibitor and corresponding methods of preparation thereof, wherein the Cot inhibitor has the following formula:
PROCESS FOR PREPARING A COT INHIBITOR COMPOUND
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Paragraph 0371; 0416; 0422; 0424, (2021/10/11)
Disclosed are syntheses of a Cot (cancer Osaka thyroid) inhibitor, which has the formula (I).
COT MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 159, (2017/01/26)
The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
