70837-27-3Relevant academic research and scientific papers
FLUORINATED QUINOLINE AND QUINOXALINE DERIVATIVES AS DIHYDROOROTATE DEHYDROGENASE (DHODH) INHIBITORS FOR THE TREATMENT OF CANCER, AUTOIMMUNE AND INFLAMMATORY DISEASES
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Page/Page column 78, (2021/05/07)
The present invention discloses compounds formula (I): (I) wherein X is CH; The present compounds of formula (I) are dihydroorotate dehydrogenase (DHODH) inhibitors, and are useful for the treatment of inflammatory disorders, autoimmune disorders and cancer, such as e.g. lymphomas, leukemias, carcinomas, and sarcomas. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 60 to 136; examples 1 to 39; tables 1 and 2). An exemplary compound is e.g. : 4-ethyl-1-(7-fluoro-4-isopropyl-2- (2-methoxyphenyl)quinolin-6-yl)-3-(hydroxymethyl)-1H-1,2,4- triazol-5(4H)-one (example 1): (AA)
Gold(I)-Catalyzed Cascade Cyclization Reactions of Allenynes for the Synthesis of Fused Cyclopropanes and Acenaphthenes
Ikeuchi, Takaya,Inuki, Shinsuke,Oishi, Shinya,Ohno, Hiroaki
supporting information, p. 7792 - 7796 (2019/05/15)
A gold-catalyzed reaction of phenylene-tethered allenynes with benzofurans gave 1-(naphth-1-yl)cyclopropa[b]benzofuran derivatives, whereas the reaction of 1-allenyl-2-ethynyl-3-methylbenzene derivatives in the absence of benzofurans gave acenaphthenes in good yields. These results can be rationalized by nucleophilic attack of the alkyne moiety on an activated allene to form a vinyl cation intermediate.
Method for catalytic conversion of cyano group into deuterated methyl, prepared aromatic deuterated methyl compound and application of compound
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Paragraph 0074; 0075; 0076; 0077; 0078, (2017/12/09)
The invention provides a method for catalytic conversion of a cyano group into deuterated methyl, a prepared aromatic deuterated methyl compound and an application of the compound. The method comprises the steps as follows: an aromatic cyano compound reacts to produce the aromatic deuterated methyl compound under the action of a metal catalyst with deuterium gas serving as a deuterium source. The cyano group is directly catalyzed into deuterated methyl with the deuterium gas serving as the deuterium source, the operation is simple, the raw material is cheap and easy to obtain, the reaction yield is high, the product deuteration rate is high, and the method can be applied to mass production. The prepared aromatic deuterated methyl compound can be used as a deuterated medicine or can be used for preparation of a deuterated medicine or deuterated medicine composition, and the pharmacokinetics, pharmacodynamics or metabolism toxicity of the medicine can be reduced while the medicine molecular activity is kept unchanged basically.
Active site dynamics of toluene hydroxylation by cytochrome P-450
Hanzlik,Ling
, p. 3992 - 3997 (2007/10/02)
Rat liver cytochrome P-450 hydroxylates toluene to benzyl alcohol plus o-, m-, and p-cresol. Deuterated toluenes (C6D5CH3, C6D5CD3, PhCD(n)H(3-n)) were incubated under saturating conditions
