5336-76-5Relevant academic research and scientific papers
Design, Synthesis, and Structure-Activity Relationship Study of Pyrazolones as Potent Inhibitors of Pancreatic Lipase
Zhang, Jing,Yang, Yang,Qian, Xing-Kai,Song, Pei-Fang,Zhao, Yi-Shu,Guan, Xiao-Qing,Zou, Li-Wei,Bao, Xiaoze,Wang, Hong
supporting information, p. 1600 - 1604 (2021/03/03)
Pancreatic lipase (PL), a key target for the prevention and treatment of obesity, plays crucial roles in the hydrolysis and absorption of in dietary fat. In this study, a series of pyrazolones was synthesized, and their inhibitory effects against PL were
Discovery of pyrazolones as novel carboxylesterase 2 inhibitors that potently inhibit the adipogenesis in cells
Qian, Xing-Kai,Zhang, Jing,Song, Pei-Fang,Zhao, Yi-Su,Ma, Hong-Ying,Jin, Qiang,Wang, Dan-Dan,Guan, Xiao-Qing,Li, Shi-Yang,Bao, XiaoZe,Zou, Li-Wei
, (2021/05/10)
Carboxylesterase 2 (CES2) is one of the most important Phase I drug metabolizing enzymes in the carboxylesterase family. It plays crucial roles in the bioavailability of oral ester prodrugs and the therapeutic effect of some anticancer drugs such as irino
Palladium Catalyzed Ring Expansion Reaction of Isoxazolones with Isocyanides: Synthesis of 1,3-Oxazin-6-One Derivatives
Zhu, Yi-Ming,Zhang, Wan,Li, Hongkun,Xu, Xiao-Ping,Ji, Shun-Jun
, p. 808 - 818 (2020/12/03)
A palladium catalyzed ring expansion reaction of isoxazolones with isocyanides was disclosed. In the reaction, a cascade process involving ring-opening/cyclization was suggested. The reaction features high atomic economy due to no elimination of CO2 occurred. Moreover, products obtained demonstrate aggregation-induced emission properties with relatively high solid-state emission efficiencies. (Figure presented.).
Radical Chlorodifluoromethylation: Providing a Motif for (Hetero)arene Diversification
McAtee, Rory C.,Beatty, Joel W.,McAtee, Christopher C.,Stephenson, Corey R. J.
, p. 3491 - 3495 (2018/06/26)
A method for the radical chlorodifluoromethylation of (hetero)arenes using chlorodifluoroacetic anhydride is reported. This operationally simple protocol proceeds under mild photochemical conditions with high functional group compatibility and complements the large body of literature for the trifluoromethylation of (hetero)arenes. Introduction of the chlorodifluoromethyl motif enables rapid diversification to a wide array of aromatic scaffolds. This work showcases the chlorodifluoromethyl group as an attractive entryway to otherwise synthetically challenging electron-rich difluoromethyl(hetero)arenes. Furthermore, facile conversion of the CF2Cl moiety into the corresponding aryl esters, gem-difluoroenones, and β-keto-esters is demonstrated.
Rhodium-catalyzed hydroaroylation of α,β-unsaturated esters using aroyl chlorides and Et2MeSiH
Muraoka, Takako,Hiraiwa, Eiji,Abe, Minami,Ueno, Keiji
supporting information, p. 4309 - 4312 (2013/07/26)
Hydroaroylation of methyl acrylate 2a to give the α-aroyl esters 4 took place in the three-component reaction of 2a, aroyl chlorides 1, and Et 2MeSiH in the presence of 1 mol % of [Rh(cod)(PR3) 2]OTf (cod = 1,5-cyclooctadi
Reductive Reformatsky-Honda reaction of α,β-unsaturated esters: Facile formation of 1,3-dicarbonyl compounds and β-hydroxy esters
Sato, Kazuyuki,Isoda, Motoyuki,Ohata, Shizuka,Morita, Shuhei,Tarui, Atsushi,Omote, Masaaki,Kumadaki, Itsumaro,Ando, Akira
supporting information; experimental part, p. 510 - 514 (2012/04/23)
The reaction of tris(triphenylphosphine)rhodium chloride [RhCl(PPh 3)3] with diethylzinc (Et2Zn) easily afforded a rhodium-hydride complex that effects the 1,4-reduction of α,β- unsaturated esters to give rhodium enolates. Formation of the rhodium enolate is followed by transmetalation with the zinc species to give a Reformatsky-type reagent, and this reacts with various acid chlorides at the α-position to give β-keto esters. The Reformatsky-type reagent also reacts with various electrophiles such as aldehydes, ketones and acid anhydrides to give the corresponding products in which the electrophiles were introduced reductively at the α-position of α,β-unsaturated esters. Copyright
Stereoselective reduction of 2-methyl-3-oxo esters (or amides) with sodium borohydride catalyzed by manganese (II) chloride or tetrabutylammonium borohydride. A practical preparation of erythro and threo-3-hydroxy-2-methyl esters (or amides)
Taniguchi, Masahiko,Fujii, Hideaki,Oshima, Koichiro,Utimoto, Kiitiro
, p. 11169 - 11182 (2007/10/02)
erythro-3-Hydroxy-2-methylpropionates or erythro-3-hydroxy-2-methylpropionamides were prepared with high stereoselectivity by NaBH4 reduction of the corresponding 2-methyl-3-oxo esters or 2-methyl-3-oxo amides in the presence of a catalytic amount of manganese(II) chloride. On the other hand, reduction of these substrates with n-Bu4NBH4 provided threo-isomers selectively. erythro-Selective reduction of 2-methyl-3-oxo amides with NaBH3CN in 1N HCl-MeOH is also described.
Reactions of Trimethylsilyl Ketene Acetals with Benzoyl Cyanide and with α-Keto Esters
Reddy, Chaganti P.,Tanimoto, Shigeo
, p. 411 - 414 (2007/10/02)
Trimethylsilyl ketene acetals reacted with benzoyl cyanide in the absence of a catalyst to give N-trimethylsilyl-β-benzoyl-β-iminopropionates.In the presence of a Lewis acid catalyst they gave the corresponding α-benzoylcarboxylates in moderate yields.Sev
