87657-76-9Relevant academic research and scientific papers
Migratory Reductive Acylation between Alkyl Halides or Alkenes and Alkyl Carboxylic Acids by Nickel Catalysis
He, Jun,Song, Peihong,Xu, Xianfeng,Zhu, Shaolin,Wang, You
, p. 3253 - 3259 (2019)
A mild migratory reductive acyl cross-coupling has been achieved through NiH-catalyzed chainwalking and subsequent cross-coupling from two abundant starting materials, alkyl bromides, and carboxylic acids. This strategy allows the direct acylation of the
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes
Wang, Congcong,Zhang, Yu-Fang,Guo, Shimeng,Zhao, Quan,Zeng, Yanping,Xie, Zhicheng,Xie, Xin,Lu, Boxun,Hu, Youhong
, p. 941 - 957 (2020/11/30)
GPR52 is an orphan G protein-coupled receptor (GPCR) that has been recently implicated as a potential drug target of Huntington's disease (HD), an incurable monogenic neurodegenerative disorder. In this research, we found that striatal knockdown of GPR52 reduces mHTT levels in adult HdhQ140 mice, validating GPR52 as an HD target. In addition, we discovered a highly potent and specific GPR52 antagonist Comp-43 with an IC50 value of 0.63 μM by a structure-activity relationship (SAR) study. Further studies showed that Comp-43 reduces mHTT levels by targeting GPR52 and promotes survival of mouse primary striatal neurons. Moreover, in vivo study showed that Comp-43 not only reduces mHTT levels but also rescues HD-related phenotypes in HdhQ140 mice. Taken together, our study confirms that inhibition of GPR52 is a promising strategy for HD therapy, and the GPR52 antagonist Comp-43 might serve as a lead compound for further investigation.
Manganese-Catalyzed Hydroarylation of Unactivated Alkenes
Liu, Ting,Wang, Congyang,Yang, Yunhui
supporting information, p. 14256 - 14260 (2020/07/13)
Transition-metal-catalyzed hydroarylation of unactivated alkenes with strategic use of remote coordinating functional groups has received significant attention recently to address the issues of both low reactivity and poor selectivity. The bidentate 8-aminoquinoline amide group is the most successfully adopted in unactivated alkenes for Pd and Ni catalysis. We describe the first manganese-catalyzed hydroarylation of unactivated alkenes bearing diverse simple functionalities with arylboronic acids. A series of δ- and γ-arylated amides, ketones, pyridines, and amines was accessed with excellent regioselectivity and in high yields. Hydroalkenylation of unactivated alkenes was also shown to be applicable under this manganese-catalysis regime. The method features earth-abundant manganese catalysis, easily available substrates, broad functional-group tolerance, and excellent regioselective control.
Preparation and catalytic application of Pd loaded titanate nanotube: Highly selective α alkylation of ketones with alcohols
Jang, Jum Suk,Kwon, Min Serk,Kim, Hyun Gyu,Park, Jae Wook,Lee, Jae Sung
experimental part, p. 1617 - 1621 (2012/07/14)
The titanate nanotube (TNT) was hydrothermally synthesized in 10 M NaOH aqueous solution at 150 °C for 72 h. Titanate nanotube with high surface area (292 m2/g) is a good candidate as a support for catalytic reaction or organic synthesis. Palladium nanoparticles with an average size of ca. 3 nm were well dispersed onto the surface of TNT nanotubes. Palladium loaded catalyst with high surface area shows a highly efficient a alkylation of ketones with primary alcohols.
Diarylheptanoids, new phytoestrogens from the rhizomes of Curcuma comosa: Isolation, chemical modification and estrogenic activity evaluation
Suksamrarn, Apichart,Ponglikitmongkol, Mathurose,Wongkrajang, Kanjana,Chindaduang, Anon,Kittidanairak, Suthadta,Jankam, Aroon,Yingyongnarongkul, Boon-ek,Kittipanumat, Narin,Chokchaisiri, Ratchanaporn,Khetkam, Pichit,Piyachaturawat, Pawinee
, p. 6891 - 6902 (2008/12/22)
Three new diarylheptanoids, a 1:2 mixture of (3S)- and (3R)-1-(4-methoxyphenyl)-7-phenyl-(6E)-6-hepten-3-ol (13a and 13b) and 1-(4-hydroxyphenyl)-7-phenyl-(6E)-6-hepten-3-one (15), together with two synthetically known diarylheptanoids 1,7-diphenyl-(1E,3E,5E)-1,3,5-triene (9) and 1-(4-hydroxyphenyl)-7-phenyl-(4E,6E)-4,6-heptadien-3-one (16), and nine known diarylheptanoids, 2, 8, 10-12, 14, a 3:1 mixture of 17a and 17b, and 18, were isolated from the rhizomes of Curcuma comosa Roxb. The absolute stereochemistry of the isolated compounds has also been determined using the modified Mosher's method. The isolated compounds and the chemically modified analogues were evaluated for their estrogenic-like transcriptional activity using RT-PCR in HeLa cell line. Some of the isolated diarylheptanoids and their modified analogues exhibited estrogenic activity comparable to or higher than that of the phytoestrogen genistein. Based on the transcriptional activation of both estrogenic targets, Bcl-xL and ERβ gene expression, the structural features for a diarylheptanoid to exhibit high estrogenic activity are the presence of an olefinic function conjugated with the aromatic ring at the 7-position, a keto group at the 3-position, and a phenolic hydroxyl group at the p-position of the aromatic ring attached to the 1-position of the heptyl chain.
Ruthenium-catalyzed regioselective α-alkylation of ketones with primary alcohols
Cho, Chan Sik,Kim, Bok Tae,Kim, Tae-Jeong,Chul Shim, Sang
, p. 7987 - 7989 (2007/10/03)
Ketones are regioselectively alkylated with an array of primary alcohols in dioxane at 80°C in the presence of a catalytic amount of a ruthenium catalyst together with KOH and a hydrogen acceptor.
Synthesis of diarylheptanoids and assessment of their pungency
Itokawa,Aiyama,Ikuta
, p. 2491 - 2496 (2007/10/02)
With the aim of correlating pungency with substituent groups on one benzene ring, various analogues of yakuchinones were synthesized by means of the Claisen-Schmidt reaction. Their pungencies were assessed by direct comparison of the threshold concentrations obtained in taste experiments. The presence of a phenolic hydroxyl group was indispensable for high pungency, while that of a 1,2-double bond of the heptanone part tended to decrease the pungency.
