352226-74-5Relevant articles and documents
Treatment method of by-product after enzymatic resolution of gamma-lactam
-
Paragraph 0014-0017, (2021/02/10)
The invention provides a treatment method of a by-product after enzymatic resolution of gamma-lactam. The treatment method comprises the following steps of carrying out racemization catalytic reactionon the by-product (+)1-amino-4-formate-2-cyclopentene,
Access to 1′-Amino Carbocyclic Phosphoramidite to Enable Postsynthetic Functionalization of Oligonucleotides
Rydzik, Anna M.,Balk, Regina,Koegler, Martin,Steinle, Tobias,Riether, Doris,Gottschling, Dirk
supporting information, p. 6735 - 6739 (2021/09/11)
We report a synthesis of a carbocyclic, abasic RNA phosphoramidite decorated with an amino functionality. The building block was efficiently incorporated into an RNA oligonucleotide in a site-specific manner, followed by deprotection to a free amino group
Diastereoselective Diboration of Cyclic Alkenes: Application to the Synthesis of Aristeromycin
Vendola, Alex J.,Allais, Christophe,Dechert-Schmitt, Anne-Marie R.,Lee, James T.,Singer, Robert A.,Morken, James P.
supporting information, p. 2863 - 2867 (2021/05/05)
The Pt-catalyzed diboration of cyclic alkenes is extended to unsaturated heterocycles and bicyclic compounds and can be accomplished in a diastereoselective fashion. The optimal procedures, substrate scope, and diastereoselectivity were investigated, and examples employing both homogeneous and heterogeneous catalysis were examined. Lastly, application to the construction of the nucleoside analog (±)-aristeromycin was conducted.
Pyrimido triazole compound and medical application thereof (by machine translation)
-
Paragraph 0043; 0045-0047, (2020/05/30)
The present invention relates to a compound of general (I) or a hydrate thereof or a pharmaceutically acceptable salt, thereof, a hydrate thereof or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the same or a pharmaceutically acceptable salt thereof, and use, of the compound or a pharmaceutically acceptable salt thereof in the manufacture of a medicament . The medicament is for anti-platelet aggregation and treatment of related diseases such as antithrombotic . (by machine translation)
Substituent and solvent effects in the 1,3-dipolar cycloadditions for synthesis of anti-influenza agent peramivir and its analog
Chen, Chien-Liang,Chiu, Tzu-Wei,Chen, Yung-Wen,Fang, Jim-Min
, p. 4458 - 4470 (2019/07/03)
Influenza remains a health problem to humans. Peramivir is a FDA approved anti-influenza drug targeting the virus neuraminidase. The (3 + 2) cycloaddition reaction of 2-ethylbutanenitrile oxide with the cyclopentene dipolarophile derived from Vince lactam is a key step in the conventional synthesis of peramivir. Our study showed that conducting the (3 + 2) cycloaddition reactions with either aliphatic or aromatic nitrile oxide in hexane solution provided high percentage of the desired regioisomer, and the N-substituent having electron-withdrawing property is also beneficial to the regioselectivity. This study also demonstrated an alternative synthetic pathway of (?)-peramivir and the analog having a phenyl group in place of the 3-pentyl moiety.
Discovery and SAR of 5-aminooctahydrocyclopentapyrrole-3a-carboxamides as potent CCR2 antagonists
Cai, Chaozhong,McComsey, Dave F.,Hou, Cuifen,O'Neill, John C.,Opas, Evan,McKenney, Sandra,Johnson, Dana,Sui, Zhihua
, p. 1239 - 1242 (2014/03/21)
SAR study of 5-aminooctahydrocyclopentapyrrole-3a-carboxamide scaffold led to identification of several CCR2 antagonists with potent activity in both binding and functional assays. Their cardiovascular safety and pharmacokinetic properties were also evalu
CHEMOKING RECEPTOR ANTAGONISTS
-
Page/Page column 155, (2013/03/26)
Disclosed herein are chemokine receptor antagonists of formula (I) wherein G1, X1, X2, and X3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
Syntheses and evaluation of fluorinated conformationally restricted analogues of GABA as potential inhibitors of GABA aminotransferase
Wang, Zhiyong,Silverman, Richard B.
, p. 2242 - 2252 (2007/10/03)
Inhibition of γ-aminobutyric acid aminotransferase (GABA-AT) could raise the concentration of GABA, an inhibitory neurotransmitter in the human brain, and could have therapeutic applications for a variety of neurological diseases including epilepsy. Four fluorine-containing analogues of GABA with conformations restricted by a cyclohexane ring system were designed and synthesized, but unlike some of their five-membered ring counterparts, minimal inhibition of GABA-AT was observed. It is likely that the rigid chair conformation of these compounds cannot be accommodated well in the enzyme's active site.
Ruthenium-catalyzed rom-RCM of cyclopentene-yne. concise synthesis of a pyrrolizidine derivative
Wakamatsu, Hideaki,Sato, Yoshihiro,Fujita, Reiko,Mori, Miwako
, p. 89 - 93 (2007/10/03)
ROM-RCM (Ring-Opening Metathesis and Ring-Closing Metathesis) of cyclopentene-yne having an ester moiety was demonstrated using first- and second-generation Grubbs' catalysts. When the reaction of cycloalkene-yne was carried out in the presence of 5 mol %
PRODUCTION METHOD FOR CIS-1-AMINO-4-HYDROXYMETHYL-2-CYCLOPENTENE OR ITS SALT
-
Page/Page column 15, (2010/02/14)
PROBLEM TO BE SOLVED: To provide a method capable of producing cis-1-amino-4-hydroxymethyl-2-cyclopentene or its salt with high selectivity and a high yield by using inexpensive reactants easily handleable. SOLUTION: Cis-1-amino-4-hydroxymethyl-2-cyclopentene represented by formula (II) or its salt is produced by mixing a cis-4-amino-2-cyclopentene-1-carboxylic ester salt represented by general formula (I) (wherein R1 is an optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, or aralkyl group; and A is an inorganic or organic acid residue) with a metal boron hydride complex compound under the condition that the stoichiometric ratio of the amount of the metal boron hydride complex compound to the amount of the cis-4-amino-2-cyclopentene-1-carboxylic ester salt is 1-10. COPYRIGHT: (C)2006,JPOandNCIPI