71785-96-1Relevant academic research and scientific papers
A Spiroalkylation Method for the Stereoselective Construction of α-Quaternary Carbons and Its Application to the Total Synthesis of (R)-Puraquinonic Acid
Elmehriki, Adam A. H.,Gleason, James L.
, p. 9729 - 9733 (2019/12/02)
Cyclic α-quaternary carbon stereocenters were prepared from biselectrophillic substrates and an easily prepared chiral bicyclic sulfonyl lactam. This was achieved in two steps by spiroalkylation, employing biphasic reaction conditions with a phase-transfer catalyst, followed by reduction and alkylation with a series of alkyl halide electrophiles. The products of this method were isolated in good yields with with high levels of diastereoselectivity. This methodology was employed in the enantioselective total synthesis of (R)-puraquinonic acid (1) for a late-stage installation of the α-quaternary carbon stereocenter. This enabled the shortest synthesis of 1 to date, an eight-pot sequence providing an overall yield of 14%.
As neuroprotective agents of pharmaceutical compounds
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Paragraph 0580; 0581; 0582; 0583; 0597; 0598; 0599; 0600, (2019/06/26)
The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
Tyrosine Kinase Inhibitor And Uses Thereof
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Paragraph 0463-0464, (2017/05/15)
Disclosed is a compound of Formula (I) or a pharmaceutically acceptable salt, ester, or solvate thereof, or their stereoisomers, which can be used as tyrosine kinase inhibitor. Also disclosed is a method for preparing the compound, a pharmaceutical composition and a kit comprising the compound, and uses of the compound. The compound can be used as tyrosine kinase inhibitor, or can be used to reduce or inhibit activity of EGFR or mutant thereof, such as EGFR mutant comprising T790M mutation, in a cell, or to treat and/or prevent a disease associated with overactivity of EGFR, such as cancer.
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase
Gingrich, Diane E.,Lisko, Joseph G.,Curry, Matthew A.,Cheng, Mangeng,Quail, Matthew,Lu, Lihui,Wan, Weihua,Albom, Mark S.,Angeles, Thelma S.,Aimone, Lisa D.,Haltiwanger, R. Curtis,Wells-Knecht, Kevin,Ott, Gregory R.,Ghose, Arup K.,Ator, Mark A.,Ruggeri, Bruce,Dorsey, Bruce D.
experimental part, p. 4580 - 4593 (2012/07/28)
Anaplastic lymphoma kinase (ALK) is a promising therapeutic target for the treatment of cancer, supported by considerable favorable preclinical and clinical activities over the past several years and culminating in the recent FDA approval of the ALK inhib
Development and scale-up of an optimized route to the ALK inhibitor CEP-28122
Allwein, Shawn P.,Roemmele, Renee C.,Haley, James J.,Mowrey, Dale R.,Petrillo, Daniel E.,Reif, James J.,Gingrich, Diane E.,Bakale, Roger P.
scheme or table, p. 148 - 155 (2012/05/20)
Evolution of the process strategies to prepare CEP-28122, an anaplastic lymphoma kinase (ALK) inhibitor, is presented. The initial medicinal chemistry route, used for the preparation of key supplies for biological screening, is reviewed. In addition, the
10A-AZALIDE COMPOUND HAVING 4-MEMBERED RING STRUCTURE
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Page/Page column 41, (2011/04/14)
A 10a-azalide compound having a 4-membered ring structure crosslinked at the 10a- and 12-positions, which is represented by the formula (I), and is effective on even Haemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
SAR studies of capsazepinoid bronchodilators. Part 1: The importance of the catechol moiety and aspects of the B-ring structure
Dalence-Guzman, Maria F.,Berglund, Magnus,Skogvall, Staffan,Sterner, Olov
, p. 2499 - 2512 (2008/09/21)
Capsazepine as well as its derivatives and analogues are general inhibitors of constriction of human small airways. From a systematic variation of the capsazepine structure, divided into four regions, SARs were established. This part concerns the catechol moiety of the A-ring as well as the 2,3,4,5-tetrahydro-1H-2-azepine moiety (the B-ring) of capsazepine. It is revealed that a conformational constrain (as a fused ring) is important and that compounds with a six-membered B-ring (as a 1,2,3,4-tetrahydroisoquinoline) in general are more potent than the corresponding isoindoline, 2,3,4,5-tetrahydro-1H-2-benzazepine and 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.
Inhibitors of phenylalanine ammonia-lyase: Substituted derivatives of 2-aminoindane-2-phosphonic acid and 1-aminobenzylphosphonic acid
Miziak, Piotr,Zon, Jerzy,Amrhein, Nikolaus,Gancarz, Roman
, p. 407 - 415 (2007/10/03)
Six derivatives of 2-aminoindane-2-phosphonic acid and 1-aminobenzylphosphonic acid were synthesized. The compounds were tested both as inhibitors of buckwheat phenylalanine ammonia-lyase (in vitro) and as inhibitors of anthocyanin biosynthesis (in vivo). (±)-2-Amino-4-bromoindane-2-phosphonic acid was found to be the strongest inhibitor from investigated compounds. The results obtained are a basis for design of phenylalanine ammonia-lyase inhibitors useful in the enzyme structure studies in photo labelling experiments.
AZACYCLIC COMPOUNDS AS INHIBITORS OF SENSORY NEURONE SPECIFIC CHANNELS
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Page 63-64, (2010/02/10)
Compounds of the formula (I), and pharmaceutically acceptable salts thereof, are found to be antagonists of SNS sodium channels. They are therefore useful as analgesic and neuroprotective agents wherein: X is -N- or -CH-; n is from 0 to 3.
Synthesis of puraquinonic acid ethyl ester and deliquinone via a common intermediate
Kraus, George A.,Choudhury, Prabir K.
, p. 5857 - 5859 (2007/10/03)
Both compounds were prepared via a common intermediate. The key features included the direct synthesis of the indan skeleton and the radical addition to a quinone.
