19444-23-6Relevant articles and documents
Synthesis and Applications of Unquaternized C-Bound Boron Enolates
Ng, Elvis Wang Hei,Low, Kam-Hung,Chiu, Pauline
, p. 3537 - 3541 (2018/03/21)
A general and facile method to prepare unquaternized C-bound boron enolates by a ligand-controlled O-to-C isomerization is reported. Using this protocol, C-bound pinacolboron enolates have been isolated in pure form for the first time, and have been fully characterized by NMR spectroscopy and X-ray crystallography. In contrast to the general perception, such C-boron enolates are stable without coordinative saturation at the boron. Moreover, C-boron enolates present reactivities that are distinct from the O-boron enolates, and their applications in C-O and C-C bond formations are demonstrated.
O-Benzylation of Carboxylic Acids Using 2,4,6-Tris(benzyloxy)-1,3,5-triazine (TriBOT) under Acidic or Thermal Conditions
Yamada, Kohei,Yoshida, Saki,Fujita, Hikaru,Kitamura, Masanori,Kunishima, Munetaka
, p. 7997 - 8002 (2015/12/24)
Two methods for the synthesis of benzyl esters from carboxylic acids using the O-benzylating reagent 2,4,6-tris(benzyloxy)-1,3,5-triazine (TriBOT) have been developed. The reactions were conducted either in the presence of a catalytic amount of TfOH at room temperature (acidic conditions) or in the absence of TfOH at 180-230 C (thermal conditions). Interestingly, the O-benzylation of hydroxy carboxylic acids under the two conditions afforded different products: The dibenzylated product under acidic conditions and the hydroxy ester under thermal conditions. In addition to these results, other evidence indicated that the former reaction proceeds through an SN1-type mechanism, and the latter by an SN2-type mechanism. Two methods for the O-benzylation of carboxylic acids using TriBOT have been developed under either acidic or thermal conditions. The O-benzylation of hydroxy carboxylic acids afforded the dibenzylated product under acidic conditions and the hydroxy ester under thermal conditions. The former reaction proceeds through an SN1-type mechanism and the latter by an SN2-type mechanism.
Versatile and sustainable alcoholysis of amides by a reusable CeO 2 catalyst
Siddiki, S. M. A. Hakim,Touchy, Abeda Sultana,Tamura, Masazumi,Shimizu, Ken-Ichi
, p. 35803 - 35807 (2014/11/07)
CeO2 catalyzed the esterification between an equivalent molar ratio of primary amides and alcohols under neutral conditions, which provides the first versatile reusable catalytic system for direct alcoholysis of amides to esters with wider scope and 67 times higher turnover number (TON) than previous catalytic systems.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 1009, (2013/04/10)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 266, (2013/04/13)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
TREATMENT OF METABOLIC SYNDROME WITH NOVEL AMIDES
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Page/Page column 81, (2009/07/17)
The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.
PENEM PRODRUGS
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Page/Page column 19, (2008/06/13)
Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.
Synthesis of stable analogs in blood and conformational analysis of arenastatin A, a potent cytotoxic spongean depsipeptide
Murakami, Nobutoshi,Tamura, Satoru,Wang, Weiqi,Takagi, Tatsuya,Kobayashi, Motomasa
, p. 4323 - 4336 (2007/10/03)
In order to produce stable analogs in blood of arenastatin A, a potent cytotoxic depsipeptide from the marine sponge Dysidea arenaria, we synthesized four analogs in which the 15-20 ester linkage was modified. Among them, the carba analog and 20-deoxo analog showed stability in serum. The conformation of arenastatin A and its three analogs were analyzed by distance-restrained molecular dynamic calculation to elucidate a three-dimensional stereostructure contributing to the extremely potent cytotoxicity of arenastatin A.
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents
O'Connell, Celeste E.,Salvato, Kathleen A.,Meng, Zhaoyang,Littlefield, Bruce A.,Schwartz, C. Eric
, p. 1541 - 1546 (2007/10/03)
The marine natural product hapalosin and 22 analogs, which incorporated systematic substituent deletions or variations, were prepared. These compounds were evaluated in a cell-based assay for both MDR-reversing activity and general cytotoxicity. Some substituent modifications resulted in lower cytotoxicities, but most structural changes were either detrimental to or did not seriously alter the MDR-reversing activity.
Substituted azetidinones as anti-inflammatory and antidegenerative agents
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, (2008/06/13)
New substituted azetidinones of the general formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described. STR1