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.
Controlled Reduction of Carboxamides to Alcohols or Amines by Zinc Hydrides
Ong, Derek Yiren,Yen, Zhihao,Yoshii, Asami,Revillo Imbernon, Julia,Takita, Ryo,Chiba, Shunsuke
supporting information, p. 4992 - 4997 (2019/03/13)
New protocols for controlled reduction of carboxamides to either alcohols or amines were established using a combination of sodium hydride (NaH) and zinc halides (ZnX2). Use of a different halide on ZnX2 dictates the selectivity, wherein the NaH-ZnI2 system delivers alcohols and NaH-ZnCl2 gives amines. Extensive mechanistic studies by experimental and theoretical approaches imply that polymeric zinc hydride (ZnH2)∞ is responsible for alcohol formation, whereas dimeric zinc chloride hydride (H?Zn?Cl)2 is the key species for the production of amines.
VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS
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Paragraph 0268; 0269, (2018/06/23)
FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
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.
Robust cobalt oxide catalysts for controllable hydrogenation of carboxylic acids to alcohols
Song, Song,Wang, Dong,Di, Lu,Wang, Chuanming,Dai, Weili,Wu, Guangjun,Guan, Naijia,Li, Landong
, p. 250 - 257 (2018/02/20)
The selective catalytic hydrogenation of carboxylic acids is an important process for alcohol production, while efficient heterogeneous catalyst systems are still being explored. Here, we report the selective hydrogenation of carboxylic acids using earth-abundant cobalt oxides through a reaction-controlled catalysis process. The further reaction of the alcohols is completely hindered by the presence of carboxylic acids in the reaction system. The partial reduction of cobalt oxides by hydrogen at designated temperatures can dramatically enhance the catalytic activity of pristine samples. A wide range of carboxylic acids with a variety of functional groups can be converted to the corresponding alcohols at a yield level applicable to large-scale production. Cobalt monoxide was established as the preferred active phase for the selective hydrogenation of carboxylic acids.
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.
Photochemical Homologation for the Preparation of Aliphatic Aldehydes in Flow
Chen, Yiding,Leonardi, Marco,Dingwall, Paul,Labes, Ricardo,Pasau, Patrick,Blakemore, David C.,Ley, Steven V.
, p. 15558 - 15568 (2019/01/04)
Cheap and readily available aqueous formaldehyde was used as a formylating reagent in a homologation reaction with nonstabilized diazo compounds, enabled by UV photolysis of bench-stable oxadiazolines in a flow photoreactor. Various aliphatic aldehydes were synthesized along with the corresponding derivatized alcohols and benzimidazoles. No transition-metal catalyst or additive was required to affect the reaction, which proceeded at room temperature in 80 min.
OXAZOLIDINONE HYDROXAMIC ACID COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 109, (2015/05/19)
This invention pertains generally to treating bacterial infections using organic compounds of Formula I. In certain aspects, the invention pertains to treating infections caused by Gram-negative bacteria. (I) wherein X, Y, R1, R2, R3, R4 and R5 and defined herein.
SUBSTITUTED 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS
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Paragraph 0574; 0575, (2015/02/02)
The present invention relates to substituted bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
IRAK INHIBITORS AND USES THEREOF
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Paragraph 00385; 00386, (2015/04/15)
The present invention provides compounds, compositions thereof, and methods of using the same.
