- Palladium-Catalyzed Distal m-C-H Functionalization of Arylacetic Acid Derivatives
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Herein, we present m-C-H olefination on derivatives of phenylacetic acids by tethering with a simple nitrile-based template through palladium catalysis. Notably, the versatility of the method is evaluated with a wide range of phenylacetic acid derivatives for obtaining the meta-olefination products in fair to excellent yields with outstanding selectivities under mild conditions. Significantly, the present strategy is successfully exemplified for the synthesis of drugs/natural product analogues (naproxen, ibuprofen, paracetamol, and cholesterol).
- Srinivas, Dasari,Satyanarayana, Gedu
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supporting information
p. 7353 - 7358
(2021/10/01)
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- CHEMOSELECTIVE METHYLENE HYDROXYLATION IN AROMATIC MOLECULES
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A chemoselective and reactive Mn(CF3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic C—H hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.
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Paragraph 0129; 0176-0178
(2020/03/28)
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- Oxadiazole Amine Derivative Compounds as Histone Deacetylase 6 Inhibitor, and the Pharmaceutical Composition Comprising the same
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The present invention relates to a novel compound having an activity of inhibiting histone deacetylase 6 (HDAC6), an optical isomer thereof or a pharmaceutically acceptable salt thereof, a use thereof for preparation of a drug for treatment, a pharmaceutical composition comprising the same, a treatment method using the composition, and a method for preparing the same. The novel compound, an optical isomer thereof or a pharmaceutically acceptable salt thereof according to the present invention has an activity of inhibiting histone deacetylase 6 (HDAC6), and is effective for preventing or treating HDAC6-related diseases, including infectious diseases; neoplasm; endocrine, nutritional and metabolic diseases; mental and behavior disorders; nerve disorders; eye and adnexa diseases; cardiovascular diseases; respiratory diseases; digestive organ diseases; skin and subcutaneous tissue diseases; musculoskeletal and connective tissue diseases; or congenital malformation, deformation and chromosomal abnormality.COPYRIGHT KIPO 2017
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Paragraph 0224-0227
(2017/07/18)
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- Highly Diastereoselective α-Arylation of Cyclic Nitriles
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A highly diastereoselective α-arylation of cyclic nitriles has been developed via a Negishi cross-coupling of commercially available aryl, heteroaryl, and alkenyl halides with cyclobutyl nitriles in the presence of tetramethylpiperidinylzinc chloride lithium chloride (TMPZnCl-LiCl) and catalytic XPhos-Pd-G2. A variety of electronically diverse electrophiles were well tolerated, and this chemistry was further advanced with application of both cyclopropyl and cyclopentyl nitriles.
- Dalziel, Michael E.,Chen, Penghao,Carrera, Diane E.,Zhang, Haiming,Gosselin, Francis
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supporting information
p. 3446 - 3449
(2017/07/15)
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- Apatinib preparation method
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The present invention relates to an apatinib preparation method, wherein specifically an organic solvent is selected to perform refining crystallization to obtain the apatinib. The method of the present invention has advantages of simple operation and low cost, and is suitable for large-scale production.
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Paragraph 0045; 0046; 0047
(2017/04/28)
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- Hydride Reduction by a Sodium Hydride-Iodide Composite
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Sodium hydride (NaH) is widely used as a Br?nsted base in chemical synthesis and reacts with various Br?nsted acids, whereas it rarely behaves as a reducing reagent through delivery of the hydride to polar π electrophiles. This study presents a series of reduction reactions of nitriles, amides, and imines as enabled by NaH in the presence of LiI or NaI. This remarkably simple protocol endows NaH with unprecedented and unique hydride-donor chemical reactivity.
- Too, Pei Chui,Chan, Guo Hao,Tnay, Ya Lin,Hirao, Hajime,Chiba, Shunsuke
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supporting information
p. 3719 - 3723
(2016/03/26)
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- PYRIMIDONE DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
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Paragraph 0212-0213
(2014/07/22)
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- Dihydroxypyrimidine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
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The present invention relates to a compound having the general formula (Di), (Dii), or (Diii), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
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Paragraph 0211-0212
(2014/02/16)
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- Synthesis of α-Aryl nitriles through palladium-catalyzed decarboxylative coupling of cyanoacetate salts with aryl halides and triflates
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Worth its salt: The palladium-catalyzed decarboxylative coupling of the cyanoacetate salt as well as its mono- and disubstituted derivatives with aryl chlorides, bromides, and triflates is described (see scheme). This reaction is potentially useful for the preparation of a diverse array of α-aryl nitriles and has good functional group tolerance. S-Phos=2-(2,6- dimethoxybiphenyl)dicyclohexylphosphine), Xant-Phos=4,5-bis(diphenylphosphino)- 9,9-dimethylxanthene. Copyright
- Shang, Rui,Ji, Dong-Sheng,Chu, Ling,Fu, Yao,Liu, Lei
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p. 4470 - 4474
(2011/06/24)
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- Ionic liquids as catalytic green solvents for nucleophilic displacement reactions
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We demonstrate the use of room-temperature ionic liquids as a catalytic, environmentally benign solvent for the cyanide displacement on benzyl chloride, replacing phase-transfer catalyzed biphasic systems and thus eliminating the need for a volatile organic solvent and hazardous catalyst disposal.
- Wheeler,West,Liotta,Eckert
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p. 887 - 888
(2007/10/03)
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- Novel arylcycloalkanepolyalkylamines
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Novel arylcycloalkanepolyalkylamines useful as anti-psychotic, anti-ischemia, anti-stroke, anti-dementia and anti-convulsant agents. These arylcycloalkanepolyalkylamines are selective high-affinity ligands to the sigma binding-sites containing three basic units: arylcycloalkyl group, an amine group and an intermediate chain. Their preparation and use for treatment of psychoses, ischemia, stroke, dementia and convulsions are also disclosed.
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- SYNTHESIS OF CYCLOPENTANE DERIVATIVES IN THE CATHODIC ELECTROLYSIS OF COMPOUNDS WITH AN ACTIVATED METHYLENE GROUP IN THE PRESENCE OF 1,4-DIBROMOBUTANE
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The cathodic electrolysis of compounds with an activated methylene group in the presence of 1,4-dibromobutane leads to 1,1-disubstituted cyclopentanes.
- Tatarinova, V. I.,Vasil'ev, A. A.,Petrosyan, V. A.
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p. 2399 - 2401
(2007/10/02)
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- Triazole and imidazole compounds useful as plant growth regulators and fungicides
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A compound having the general formula (I): STR1 and stereoisomers thereof, wherein W is CH or N; Q is optionally substituted aryl, optionally substituted aralkyl, or alkyl; R1, R2, R3, R4, R5, R6, R7, and R8, which may be the same or different, are H, hydroxy, alkyl, cycloalkyl, optionally substituted aralkyl, or optionally substituted phenyl, or any of the pairs R1 and R2 ; R3 and R4 ; R5 and R6 ; or R7 and R8 can, together with the adjacent ring carbon atom, represent a carbonyl group (C=O); R9 and R10 which may be the same or different, are H, alkyl, cycloalkyl, optionally substituted aralkyl, or optionally substituted phenyl; n is 0 or 1; and acid salts and metal complexes thereof. The compounds have plant growth regulating and fungicidal activity.
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- Some O alkylaminoalkyl thioester analogs of adiphenine and related esters
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Syntheses of nine O alkylaminoalkyl thioester analogs of the adiphenine molecule: preliminary studies of their spasmolytic activity and of their action against the state of tremor caused by oxotremorine in the mouse are described.
- Reynaud,Richard,Menard,et al.
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p. 262 - 267
(2007/10/05)
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