301232-45-1Relevant articles and documents
Electrochemical Tandem Olefination and Hydrogenation Reaction with Ammonia
Zhang, Xiaofeng,Jiang, Runze,Cheng, Xu
, p. 16016 - 16025 (2021/08/24)
An electrochemical Horner-Wadsworth-Emmons/hydrogenation tandem reaction was achieved using ammonia as electron and proton donors. The reaction could give two-carbon-elongated ester and nitrile from aldehyde or ketones directly. This reaction could proceed with a catalytic amount of base or even without a base. The ammonia provides both the electron and proton for this tandem reaction and enables the catalyst-free hydrogenation of an α,β-unsaturated HWE intermediate. More than 40 examples were reported, and functional groups, including heterocycles and hydroxyl, were tolerated.
One-Pot, Tandem Wittig Hydrogenation: Formal C(sp3)-C(sp3) Bond Formation with Extensive Scope
Devlin, Rory,Jones, David J.,Mcglacken, Gerard P.
supporting information, p. 5223 - 5228 (2020/07/14)
A one-pot, tandem Wittig hydrogenation of aldehydes with stabilized ylides is reported, representing a formal C(sp3)-C(sp3) bond construction. The tandem reaction operates under mild conditions, is high yielding, and is broad in scope. Chemoselectivity for olefin reduction is observed, and the methodology is demonstrated in the synthesis of lapatinib analogues and a formal synthesis of (±)-cuspareine. Early insights suggest that the chemoselectivity observed in the reduction step is due to partial poisoning of the catalyst, after step one, thus adding to the power of the one-pot procedure.
ANTIMICROBIAL COMPOUNDS AND METHODS
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, (2020/07/31)
The invention is directed to compounds that are active as antibacterial agents. The invention compounds are active against gram-positive and gram-negative bacteria and can be used to treat infections caused by gram-positive and gram-negative bacteria. Also disclosed are processes and intermediates for making the compounds.
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors
Rossi, Cristina,Porcelloni, Marina,D'Andrea, Piero,Fincham, Christopher I.,Ettorre, Alessandro,Mauro, Sandro,Squarcia, Antonella,Bigioni, Mario,Parlani, Massimo,Nardelli, Federica,Binaschi, Monica,Maggi, Carlo A.,Fattori, Daniela
, p. 2305 - 2308 (2011/05/15)
We report here the strategy used in our research group to find a new class of histone deacetylase (HDAC) inhibitors. A series of N-substituted 4-alkylpiperazine and 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of HDAC inhibitors (zinc binding moiety-linker-capping group) has been designed, prepared, and tested for HDAC inhibition. Linker length and aromatic capping group connection were systematically varied to find the optimal geometric parameters. A new series of submicromolar inhibitors was thus identified, which showed antiproliferative activity on HCT-116 colon carcinoma cells.
Design, synthesis, and structure-activity relationships of potent GPIIb/IIIa antagonists: Discovery of FK419
Yamanaka, Toshio,Ohkubo, Mitsuru,Kuroda, Satoru,Nakamura, Hideko,Takahashi, Fumie,Aoki, Toshiaki,Mihara, Kayoko,Seki, Jiro,Kato, Masayuki
, p. 4343 - 4352 (2007/10/03)
The discovery of the non-peptide antiplatelet injectable agent FK419 is reported. Based on the β-turn structure of RGD peptide sequences in the α chain of fibrinogen, which binds the glycoprotein IIb/IIIa (GPIIb/IIIa) on the surface of platelets to induce
N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
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Page/Page column 24-25, (2010/11/30)
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
Ester derivatives
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Page/Page column 33, (2008/06/13)
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); 1[in which A signifies a group expressed by a formula (a0) or (b0); 2Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X?signifies an anion].
Muscarinic M3 receptor antagonists with (2R)-2-[(1R)-3,3-Difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2
Ogino, Yoshio,Ohtake, Norikazu,Kobayashi, Kensuke,Kimura, Toshifumi,Fujikawa, Toru,Hasegawa, Takuro,Noguchi, Kazuhito,Mase, Toshiaki
, p. 2167 - 2172 (2007/10/03)
Optimization of the amine part of our original muscarinic M3 receptor antagonist 1 was performed to identify M3 receptor antagonists that are superior to 1. Compounds carrying a variety of diamine moieties without hydrophobic substituent on the nitrogen atom were screened against the binding affinity for the M3 receptor and the selectivity for M3 over the M1 and M2 receptors. This process led to a 4-aminopiperidinamide (2l) with a Ki value of 5.1 nM and with a selectivity of the M3 receptor that was 46-fold greater than that of the M2 receptor. Further derivatization of 2l by inserting a spacer group or by incorporating alkyl group(s) into the amine part resulted in the identification of an 4-(aminoethyl)piperidinamide 2l-b with a Ki value of 3.7 nM for the M3 receptor and a selectivity for the M3 receptor that was 170-fold greater than that of the M2 receptor.
Pyrrolidine modulators of chemokine receptor activity
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, (2008/06/13)
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
Synthesis of substituted oxazolo[4,5-b]-pyridine derivatives
Grumel, Vale?rie,Me?rour, Jean-Yves,Guillaumet, Ge?rald
, p. 1329 - 1345 (2007/10/03)
Synthesis of new functionnalized oxazolo[4,5-b]pyridines was described. 5-Bromo-3-hydroxy-2-aminopyridine was heated, in the presence of PPSE or PPA, with 4-cyanobenzoic acid, (4-piperidinyl)acetic or propanoic acid to afford 1,3-oxazolo derivatives. Intr