142733-64-0Relevant academic research and scientific papers
Radical hydroxymethylation of alkyl iodides using formaldehyde as a C1 synthon
Caiger, Lewis,Constantin, Timothée,Douglas, James J.,Juliá, Fabio,Leonori, Daniele,Sheikh, Nadeem S.,Sinton, Conar
, p. 10448 - 10454 (2021/08/20)
Radical hydroxymethylation using formaldehyde as a C1 synthon is challenging due to the reversible and endothermic nature of the addition process. Here we report a strategy that couples alkyl iodide building blocks with formaldehyde through the use of photocatalysis and a phosphine additive. Halogen-atom transfer (XAT) from α-aminoalkyl radicals is leveraged to convert the iodide into the corresponding open-shell species, while its following addition to formaldehyde is rendered irreversible by trapping the transient O-radical with PPh3. This event delivers a phosphoranyl radical that re-generates the alkyl radical and provides the hydroxymethylated product.
Indoleamine-2,3-dioxygenase inhibitor as well as preparation method and application thereof
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, (2019/08/12)
The invention provides a compound as shown in a formula (I). The invention also relates to a pharmaceutical composition containing the compound of the formula (I) and application of the compound to preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound prepared by the method of the invention has an obvious inhibiting effect on IDO protease and is stable in metabolism in vivo. The compound or a pharmaceutical composition thereof provided by the invention can be used for preparing the IDO inhibitor drug, and can also be used for preparing medicines for preventing and/ortreating diseases with pathological characteristics of an IDO-mediated tryptophan metabolic pathway.
ISOXAZOLE β-LACTAMASE INHIBITORS
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Page/Page column 71; 72, (2013/10/21)
β-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D β-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
SYNTHESIS OF NEW CARBOCYCLIC ANALOGUES OF OXETANOCIN A AND OXETANOCIN G
Pecquet, Pascal,Huet, Francois,Legraverend, Michel,Bisagni, Emile
, p. 739 - 745 (2007/10/02)
The synthesis of cis-3-amino-1-cyclobutanemethanol has been performed in six steps (59.6percent yield) from cis-1,3-cyclobutanedicarboxylic anhydride.This allowed us to obtain two new carbocyclic analogues of oxetanocin A and oxetanocin G related to 7-deazaadenosine and 7-deazaguanosine.
