136380-18-2Relevant articles and documents
SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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, (2019/08/26)
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders as well as other disorders.
Hydrogen Bonding-Assisted Enhancement of the Reaction Rate and Selectivity in the Kinetic Resolution of d,l-1,2-Diols with Chiral Nucleophilic Catalysts
Fujii, Kazuki,Mitsudo, Koichi,Mandai, Hiroki,Suga, Seiji
supporting information, p. 2778 - 2788 (2017/08/23)
An extremely efficient acylative kinetic resolution of d,l-1,2-diols in the presence of only 0.5 mol% of binaphthyl-based chiral N,N-4-dimethylaminopyridine was developed (selectivity factor of up to 180). Several key experiments revealed that hydrogen bonding between the tert-alcohol unit(s) of the catalyst and the 1,2-diol unit of the substrate is critical for accelerating the rate of monoacylation and achieving high enantioselectivity. This catalytic system can be applied to a wide range of substrates involving racemic acyclic and cyclic 1,2-diols with high selectivity factors. The kinetic resolution of d,l-hydrobenzoin and trans-1,2-cyclohexanediol on a multigram scale (10 g) also proceeded with high selectivity and under moderate reaction conditions: (i) very low catalyst loading (0.1 mol%); (ii) an easily achievable low reaction temperature (0 °C); (iii) high substrate concentration (1.0 M); and (iv) short reaction time (30 min). (Figure presented.).
A Divergent Approach for the Synthesis of d - And l -4′-Ethynyl Dioxolane Nucleosides with Potent Anti-HIV Activity
Singh, Sarbjit,Gajulapati, Veeraswamy,Kim, Minkyoung,Goo, Ja-Il,Lee, Jae Kyun,Lee, Kyeong,Lee, Chong-Kyo,Jeong, Lak Shin,Choi, Yongseok
, p. 3050 - 3056 (2016/09/09)
Novel 4′-C-ethynyl isomeric dioxolane nucleoside analogues (β-d, α-d, β-l, and α-l, respectively) are successfully synthesized via a divergent strategy from the common starting material, (Z)-but-2-ene-1,4-diol, and are characterized and evaluated for their anti-HIV-1 and anti-HIV-2 activities. The β-d and β-l products display potent in vitro activities against HIV-1 (IIIB) with EC50 values of 0.75 and 0.87 μM, respectively, and against HIV-2 (ROD) with EC50 values of 0.75 and 0.35 μM, respectively, being better in comparison with 3TC [EC50, 5.27 μM (HIV-1) and 1.30 μM (HIV-2)]. The β-d and β-l nucleosides also potently inhibit different drug-resistant strains of the HIV-1 virus (L100I, K103N, Y181C, and V106A). The selectivity indices and cytotoxic profiles of the β-d and β-l nucleosides are much better than those of the standard drugs AZT and d4T.
12-hetero substituted 6,11-ethano-6,11-dihydrobenzo (b) quinolizinium salts and compositions and method of use thereof
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, (2008/06/13)
1-Hetero substituted 6,11-ethano-6,11-dihydrobenzo[b]quinolizinium salts, pharmaceutical compositions containing them, and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
Novel vitamin E derivatives and process for the production thereof
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, (2008/06/13)
The novel vitamin E derivative provides an excellent antihyperlipemic effect and is defined by the formula (I): STR1 wherein R represents a nicotinoyl group; and m is an integer of from 2 to 5 while n is an integer of from 3 to 6, provided that n is large