1489-97-0Relevant academic research and scientific papers
Practical Manufacture of 4-Alkyl-4-aminocyclohexylalcohols Using Ketoreductases
García-Cerrada, Susana,Redondo-Gallego, Laura,Martínez-Olid, Francisco,Rincón, Juan A.,García-Losada, Pablo
, p. 779 - 784 (2017)
The diastereoselective preparation of cis- or trans-4-substituted-4-aminocyclohexyl alcohols by conventional chemical processes reported in the literature requires long synthetic sequences and is not amenable to scale-up. In the past decade, ketoreductases (KREDs) have emerged as a powerful approach for the preparation of chiral secondary alcohols from prochiral ketones. This paper describes the diastereoselective preparation at the kilo scale of cis-allyl N-(4-hydroxy-1-methyl-cyclohexyl)carbamate (6a) via ketoreductase transformation. The methodology was also applicable to a set of different analogous cyclic ketones.
3-(dimethylaminomethyl) cyclohex-4-alcohol derivative as well as preparation method and pharmaceutical application thereof
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Paragraph 0320-0323, (2021/05/08)
The invention belongs to the field of pharmacy, and relates to a 3-(dimethylaminomethyl) cyclohex-4-alcohol derivative with a general formula (I) or a salt thereof and a preparation method, and relates to an application of the compound in treatment of opioid receptor mediated diseases. The present invention provides a pharmaceutically acceptable solvate or hydrate of a compound of formula (I), and also provides a pharmaceutical composition comprising: a compound of formula (I) or a pharmaceutically acceptable salt, solvate or hydrate thereof; and a pharmaceutically acceptable carrier. The medicine prepared from the compound can be used for treating or improving diseases related to an opioid receptor; wherein the diseases can be selected from but not limited to pain, gastrointestinal diseases and depression.
Divergent Total Syntheses of Yaequinolone-Related Natural Products by Late-Stage C-H Olefination
Ces, Sabela Vega,Fernández-Ibá?ez, M. ángeles,Jia, Wen-Liang
supporting information, p. 6259 - 6277 (2021/05/29)
Divergent total syntheses of 10 yaequinolone-related natural products have been achieved for the first time by late-stage C-H olefination of 3,4-dioxygenated 4-aryl-5-hydroxyquinolin-2(1H)-ones, core structures of this family of natural products. A robust synthetic methodology to construct the core structures has been established, and the C-H olefination reaction has been carried out with synthetically useful yields and high levels of site-selectivity under mild reaction conditions in the presence of a Pd/S,O-ligand catalyst.
CHEMICAL COMPOUNDS
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Paragraph 0266-0268, (2021/04/02)
The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as Janus kinase (JAK) inhibitors and are useful in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described herein are methods of treating inflammation, auto-immune diseases, cancer, and other conditions susceptible to inhibition of JAK by administering a compound herein described.
Ytterbium-Catalyzed Intramolecular [3 + 2] Cycloaddition based on Furan Dearomatization to Construct Fused Triazoles
Xu, Xiaoming,Zhong, Ying,Xing, Qingzhao,Gao, Ziwei,Gou, Jing,Yu, Binxun
supporting information, p. 5176 - 5181 (2020/07/14)
The 1,2,3-triazole-containing polycyclic architecture widely exists in a broad spectrum of synthetic bioactive molecules, and the development of expeditious methods to synthesize these skeletons remains a challenging task. In this work, the catalytic cyclization of biomass-derived 2-furylcarbinols with an azide to form fused triazoles is described. This approach takes advantage of a single catalyst Yb(OTf)3 and operates via a furfuryl-cation-induced intramolecular [3 + 2] cycloaddition/furan ring-opening cascade.
LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY ELEMENT
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Paragraph 0169, (2020/02/28)
PROBLEM TO BE SOLVED: To improve Δn of a liquid crystal compound. SOLUTION: One aspect of the present invention is a liquid crystal compound represented by general formula (i) [where Ri1 is a C1 to 15 alkyl group or the like, Ri2 is
HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Page/Page column 77; 78, (2019/01/17)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES
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Page/Page column 79, (2019/11/28)
Provided herein are dihydropyrimidine derivatives which are useful in the treatment of HBV infection or HBV-induced diseases, as well as pharmaceutical or medical applications thereof.
4,5,6-TRI-SUBSTITUTED INDAZOLES DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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Paragraph 0161-0162, (2019/02/19)
Provided are 4,5,6-tri-substituted indazoles derivatives, a preparation method therefor, and a use thereof in medicines. Specifically, provided are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates, or prodrugs thereof
TETRAHYDRO-IMIDAZO QUINOLINE COMPOSITIONS AS CBP/P300 INHIBITORS
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Paragraph 0085, (2019/04/11)
The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
