96149-05-2Relevant academic research and scientific papers
Development of effective bidentate diphosphine ligands of ruthenium catalysts toward practical hydrogenation of carboxylic acids
Saito, Susumu,Wen, Ke,Yoshioka, Shota
supporting information, p. 1510 - 1524 (2021/06/18)
Hydrogenation of carboxylic acids (CAs) to alcohols represents one of the most ideal reduction methods for utilizing abundant CAs as alternative carbon and energy sources. However, systematic studies on the effects of metal-to-ligand relationships on the catalytic activity of metal complex catalysts are scarce. We previously demonstrated a rational methodology for CA hydrogenation, in which CA-derived cationic metal carboxylate [(PP)M(OCOR)]+ (M = Ru and Re; P = one P coordination) served as the catalyst prototype for CA self-induced CA hydrogenation. Herein, we report systematic trial- and-error studies on how we could achieve higher catalytic activity by modifying the structure of bidentate diphosphine (PP) ligands of molecular Ru catalysts. Carbon chains connecting two P atoms as well as Ar groups substituted on the P atoms of PP ligands were intensively varied, and the induction of active Ru catalysts from precatalyst Ru(acac)3 was surveyed extensively. As a result, the activity and durability of the (PP)Ru catalyst substantially increased compared to those of other molecular Ru catalyst systems, including our original Ru catalysts. The results validate our approach for improving the catalyst performance, which would benefit further advancement of CA self-induced CA hydrogenation.
RADIOLABELED CANNABINOID RECEPTOR 2 LIGAND
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Page/Page column 15-16, (2020/01/24)
The present invention relates to a compound of formula (I) wherein R1, R2, and R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a radiolabeled ligand.
Identification and Preclinical Development of a 2,5,6-Trisubstituted Fluorinated Pyridine Derivative as a Radioligand for the Positron Emission Tomography Imaging of Cannabinoid Type 2 Receptors
Haider, Ahmed,Gobbi, Luca,Kretz, Julian,Ullmer, Christoph,Brink, Andreas,Honer, Michael,Woltering, Thomas J.,Muri, Dieter,Iding, Hans,Bürkler, Markus,Binder, Martin,Bartelmus, Christian,Knuesel, Irene,Pacher, Pal,Herde, Adrienne Müller,Spinelli, Francesco,Ahmed, Hazem,Atz, Kenneth,Keller, Claudia,Weber, Markus,Schibli, Roger,Mu, Linjing,Grether, Uwe,Ametamey, Simon M.
supporting information, p. 10287 - 10306 (2020/11/02)
Despite the broad implications of the cannabinoid type 2 receptor (CB2) in neuroinflammatory processes, a suitable CB2-targeted probe is currently lacking in clinical routine. In this work, we synthesized 15 fluorinated pyridine derivatives and tested their binding affinities toward CB2 and CB1. With a sub-nanomolar affinity (Ki for CB2) of 0.8 nM and a remarkable selectivity factor of >12,000 over CB1, RoSMA-18-d6 exhibited outstanding in vitro performance characteristics and was radiofluorinated with an average radiochemical yield of 10.6 ± 3.8% (n = 16) and molar activities ranging from 52 to 65 GBq/μmol (radiochemical purity > 99%). [18F]RoSMA-18-d6 showed exceptional CB2 attributes as demonstrated by in vitro autoradiography, ex vivo biodistribution, and positron emission tomography (PET). Further, [18F]RoSMA-18-d6 was used to detect CB2 upregulation on postmortem human ALS spinal cord tissues. Overall, these results suggest that [18F]RoSMA-18-d6 is a promising CB2 PET radioligand for clinical translation.
PYRIDINE AND PYRAZINE DERIVATIVES AS PREFERENTIAL CANNABINOID 2 AGONISTS
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Page/Page column 49; 50, (2020/01/24)
The invention relates to a compound of formula (I), wherein A1, A2 and R1-R5 are as defined in the description and in the claims. The compound of formula (I) can be used as cannabinoid 2 preferential agonist.
Asymmetric induction via metalation of succinic esters and amide using S(+) menthol and R(+) 1-Phenylethylamine as chiral auxiliaries
E Sana, Auj,Khan, Sher W.,Ambreen, Nida,Arfan, Muhammad,Zaidi, Javid H.,Khan, Khalid M.,Perveen, Shahnaz,Miana, Ghulam A.
, p. 632 - 638 (2013/02/25)
The synthesis of chiral esters and amides with the involvement of asymmetric induction by using pure chiral auxiliaries such as (1S, 2R, 5R) menthol and L-(+)-1-phenylethylamine is described. The chiral mono, di menthol esters and mono amides of succinic acid were synthesized in good yields. These esters and amides were then subjected to metalation and quenched with different alkyl halides to get α substitution to generate a new chiral center.
CYCLOPROPYL-PIPERAZINE COMPOUNDS AS CALCIUM CHANNEL BLOCKERS
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Page/Page column 24-25, (2008/06/13)
Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of compounds containing both a piperazine ring and a
Process for making monomenthyl esters
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Page/Page column 5-6, (2008/06/13)
A process for making monomenthyl esters of dicarboxylic acids is disclosed. Menthol reacts with a saturated, cyclic anhydride in the presence of a base catalyst under conditions effective to produce a mixture of mono- and bis-menthyl esters in which the molar ratio of mono- to bis-menthyl esters is enhanced compared with the ratio of esters produced in a similar uncatalyzed process.
Cyclopropane PNA: Observable triplex melting in a PNA constrained with a 3-membered ring
Pokorski, Jonathan K.,Myers, Michael C.,Appella, Daniel H.
, p. 915 - 917 (2007/10/03)
The first peptide nucleic acid (PNA) with a cyclopropane in the backbone has been synthesized, and the effects of the ring on DNA/RNA binding properties of the PNA have been examined. Well-defined triplex to duplex melting transitions of PNA2 DNA complexes is clearly observed by variable temperature UV absorbance with the cyclopropane-constrained PNA.
Halothenoyl-cyclopropane-1-carboxylic acid derivatives
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Page 9, (2010/02/07)
Compounds of formula (I) wherein R is hydroxy, linear or branched C1-C6 alkoxy, phenoxy, benzyloxy, a group -N(R1R2) wherein R1 is hydrogen, linear or branched C1-C4 alkyl, benzy
Glycoside derivatives of 2-(3,4-dichlorobenzoyl)-cycopropane-1-carboxylic acid
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Page 5, (2010/02/09)
The compounds of formula I: ???wherein R is a glycoside residue optionally having one or more hydroxy groups alkylated or acylated by C1-C4 alkyl or acyl groups, are long lasting inhibitors of kynurenine 3-monooxygenase (KMO) and potent glutamate (GLU) re
