14774-37-9Relevant articles and documents
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.
Selective Hydrogenation of Carboxylic Acids to Alcohols or Alkanes Employing a Heterogeneous Catalyst
Ullrich, Johannes,Breit, Bernhard
, p. 785 - 789 (2018/02/14)
The chemoselective hydrogenation of carboxylic acids to either alcohols or alkanes is reported, employing a heterogeneous bimetallic catalyst consisting of rhenium and palladium supported on graphite. α-Chiral carboxylic acids were hydrogenated without loss of optical purity. The catalyst displays a reverse order of reactivity upon hydrogenation of different carboxylic functions with esters being less reactive than amides and carboxylic acids. This allows for chemoselective hydrogenation of an acid in the presence of an ester or an amide function.
Aromatic-ring-containing compound, preparation method thereof, pharmaceutical composition and application thereof
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Paragraph 0691-0695, (2018/08/03)
The invention discloses an aromatic-ring-containing compound, a preparation method thereof, a pharmaceutical composition and application. The present invention provides the aromatic-ring-containing compound represented by a formula 1, a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a tautomer thereof or a solvate thereof, and the aromatic-ring-containing compound can be effectively bounded to bromodomains of BRD4, BRD3, BRD2, and BRDT in BET family to regulate transcription of downstream gene c-myc and related target genes of the c-myc so as to regulate downstream signalingpathways to play specific roles including treatment of diseases such as inflammatory diseases, cancer, and AIDS. Some of the compounds have high activity, and have good cell activity and metabolic stability, so that the compounds can be an effective drug for treating tumors.