151792-53-9Relevant articles and documents
Synthesis of enantiopure 3,5-disubstituted pyrrolidines by ring-opening/cross-metathesis reaction of 2-azanorbornene derivatives
Arjona, Odon,Cabas, Ma Jose,Nieto-Rubio, Jose,Querejeta, Ana
, p. 2079 - 2086 (2006)
A concise method for the synthesis of enantiopure 3,5-disubstituted pyrrolidines from 2-azanorbornene derivatives is described. The method is also applied to the synthesis of 3,5-disubstituted prolines.
Squarate-based carbocyclic nucleosides: Syntheses, computational analyses and anticancer/antiviral evaluation
Lu, Meijun,Lu, Qing-Bin,Honek, John F.
, p. 282 - 287 (2017)
Squaric acid and its derivatives are versatile synthons and have demonstrated applications in medicinal chemistry, notably as non-classical bioisosteric replacements for functional groups such as carboxylic acids, alpha-amino acids, urea, guanidine, peptide bonds and phosphate/pyrophosphate linkages. Surprisingly, no reports have appeared concerning its possible application as a nucleobase substitute in nucleosides. A preliminary investigation of such an application is reported herein. 3-Amino-4-((1R,4S)-4-(hydroxymethyl)cyclopent-2-en-1-yl)amino-cyclobut-3-ene-1,2-dione, 3-((1R,4S)-4-(hydroxymethyl)cyclopent-2-en-1-yl)amino-4-methoxycyclobut-3-ene-1,2-dione, and 3-hydroxy-4-((1R,4S)-4-(hydroxymethyl)cyclopent-2-en-1-yl)amino-cyclobut-3-ene-1,2-dione sodium salt were synthesized. Computational analyses of their structures and preliminary antitumor and antiviral screening results are reported.
COMPOUNDS TARGETING PRMT5
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Paragraph 0217, (2021/10/11)
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Synthesis and evaluation of cyclopentane-based muraymycin analogs targeting MraY
Kwak, Seung-Hwa,Lim, Won Young,Hao, Aili,Mashalidis, Ellene H.,Kwon, Do-Yeon,Jeong, Pyeonghwa,Kim, Mi Jung,Lee, Seok-Yong,Hong, Jiyong
, (2021/02/21)
Antibiotic resistance is one of the most challenging global health issues and presents an urgent need for the development of new antibiotics. In this regard, phospho-MurNAc-pentapeptide translocase (MraY), an essential enzyme in the early stages of peptid
COMPOUNDS TARGETING PRMT5
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Paragraph 0216, (2020/10/20)
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
PRMT5 INHIBITORS
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Page/Page column 66-67, (2020/03/02)
The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
Efficient and stereoselective synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA)
-
, (2016/06/01)
The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) from a readily available starting material (Vince lactam) in fourteen steps. An efficient and practical methodology for stereospecifi
An expedient synthesis of oxazepino and oxazocino quinazolines
Hensbergen, Albertus Wijnand,Mills, Vanessa R.,Collins, Ian,Jones, Alan M.
, p. 6478 - 6483 (2015/11/16)
A synthetic route to a new class of privileged tri- and tetra-cyclic quinazolines containing a medium-sized ring is reported. An expedient synthetic route involving nucleophilic aromatic substitution, and sequential Niementowski and BOP-mediated ring clos
Stereoselective synthesis of 2′-fluoro-6′-methylene carbocyclic adenosine via Vince lactam
Singh, Uma S.,Mishra, Ram C.,Shankar, Ravi,Chu, Chung K.
, p. 3917 - 3923 (2014/05/20)
2′-Fluoro-6′-methylene carbocyclic adenosine (FMCA) is a potent and selective inhibitor of wild type as well as drug-resistant hepatitis B virus (HBV) mutants. FMCA demonstrated excellent anti-HBV activity against both adefovir-resistant and lamivudine-re
Chemoselective opening of Vince lactam epoxide with nitrogen nucleophiles
Giorgi, Gianluca,Guideri, Luca,Ponticelli, Fabio
experimental part, p. 1463 - 1467 (2011/03/23)
Here is reported the chemoselective opening of the amide bond on a Vince lactam derivative with amines, without the cleavage of the epoxide-moiety, getting five new epoxides. Also reported is the rearrangement of the epoxides into the respective five new
