5522-92-9Relevant academic research and scientific papers
Electrochemical esterification reaction of alkynes with diols: Via cleavage of carbon-carbon triple bonds without catalyst and oxidant
Cheng, Hui-Hui,Gao, Hui,Li, Pin-Hua,Shen, Hui-Zhi,Wang, Pei-Long
supporting information, p. 6783 - 6791 (2020/11/09)
A novel electrochemical esterification of alkynes for the synthesis of esters was developed in which diols and their derivatives were used as the partners. This method is green as it is catalyst-free, oxidant-free, and additive-free and shows atom-economy. This is the first example of an electrochemical reaction via cleavage of carbon-carbon triple bonds. Meanwhile, this is also the first example of a carbon-carbon triple bond cleavage reaction of alkynes with diols. This journal is
DERIVATIVES OF RELEBACTAM AND USES THEREOF
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Paragraph 1418-1420, (2020/04/24)
Derivatives of relebactam, therapeutic methods of using the derivatives of relebactam, particularly in combination with β-lactam antibiotics and pharmaceutical compositions thereof are disclosed. The derivatives of relebactam are suitable for oral administration.
MACROCYCLIC SPIROETHERS AS MCL-1 INHIBITORS
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Paragraph 0499; 0500, (2020/07/31)
Provided are compounds represented by Formula (I-A) and the pharmaceutically acceptable salts and solvates thereof, wherein R8, R9a, R9b, R9c, R9d, X, Y, Z, Z1, W, and (aa) are as defined as set forth in the specification. Provided are also compounds of Formula (I-A) for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.
Selective Monoacylation of Diols and Asymmetric Desymmetrization of Dialkyl meso-Tartrates Using 2-Pyridyl Esters as Acylating Agents and Metal Carboxylates as Catalysts
Hashimoto, Yuki,Michimuko, Chiaki,Yamaguchi, Koki,Nakajima, Makoto,Sugiura, Masaharu
, p. 9313 - 9321 (2019/08/12)
With 2-pyridyl benzoates as acylating agents and Zn(OAc)2 as a catalyst, 1,2-diols, 1,3-diols, and catechol were selectively monoacylated. Furthermore, the highly enantioselective desymmetrization of meso-tartrates was achieved for the first time, utilizing 2-pyridyl esters and NiBr2/AgOPiv/Ph-BOX in CH3CN or CuCl2/AgOPiv/Ph-BOX in EtOAc catalyst systems (up to 96% ee). The latter catalyst system was also effective for the kinetic resolution of dibenzyl dl-tartrate.
AZTREONAM DERIVATIVES AND USES THEREOF
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Paragraph 0973; 0974; 0975; 0976; 1139; 1140, (2019/04/18)
Disclosed herein are aztreonam derivatives, therapeutic methods of using the aztreonam derivatives, particularly in combination with β-lactamase inhibitors, and pharmaceutical compositions thereof. The aztreonam derivatives can be administered orally to provide orally bioavailable aztreonam.
Beta-lactamase inhibitors and uses thereof
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Page/Page column 83, (2018/10/24)
β-Lactamase inhibiting compounds, therapeutic methods of using the β-lactamase inhibiting compounds, particularly in combination with β-lactam antibiotics and pharmaceutical compositions thereof are disclosed. The β-lactamase inhibiting compounds are suitable for oral administration.
SUBSTITUTED PYRAZOLOAZEPIN-4-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 45; 46, (2018/07/05)
The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents the treatment of inflammatory diseases and conditions.
SUBSTITUTED PYRAZOLOAZEPIN-4-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 94, (2018/07/05)
The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
Selective mono-acylation of 1,2- and 1,3-diols using (α,α- difluoroalkyl)amines
Wakita, Natsumi,Hara, Shoji
experimental part, p. 7939 - 7945 (2010/10/19)
In the reaction of N,N-diethyl-α,α-difluorobenzylamine (DFBA) with 1,2- or 1,3-diols, selective mono-benzoylation occurs to afford mono-esters of the diols in good yield. The reaction is completed under mild conditions in a short reaction time. Further, prim-, sec-, and tert-diols and catechol can be converted to the corresponding mono-benzoates. DFBA is used for the protection of the hydroxy group in sugars. The selective mono-nicotinylation, formylation and pivaloylation of diols are also performed by using the corresponding difluoroalkylamines.
EXTERNALLY MASKED NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE
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Page/Page column 45, (2009/04/24)
Masked nitrogen-substituted and oxygen-substituted neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.
