170364-89-3Relevant academic research and scientific papers
Copper-catalysed amination of alkyl iodides enabled by halogen-atom transfer
Barthelemy, Anne-Laure,Douglas, James J.,Górski, Bartosz,Juliá, Fabio,Leonori, Daniele
, p. 623 - 630 (2021/07/25)
Despite the fact that nucleophilic displacement (SN2) of alkyl halides with nitrogen nucleophiles is one of the first reactions introduced in organic chemistry teaching, its practical utilization is largely limited to unhindered (primary) or ac
ANTI-INFECTIVE HETEROCYCLIC COMPOUNDS AND USES THEREOF
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, (2019/05/22)
The present invention relates to heterocyclic compounds of Formula F-I useful as anti-infective agents. The present invention further relates to a method of treating an infection by administering such compounds, and to pharmaceutical compositions comprising such compounds.
Dearomatization-Rearomatization Strategy for Reductive Cross-Coupling of Indoles with Ketones in Water
Wang, Zemin,Zeng, Huiying,Li, Chao-Jun
supporting information, p. 2302 - 2306 (2019/04/10)
N-Alkylation of indoles is one of the important pathways for the construction of various biologically active indole molecules. Using ketones as N-alkylation reagent for indoles has been a great challenge not only because of the competing alkylation reaction of C-3 position but also because of the poor nucleophilicity of the nitrogen atom of indole, in addition to the steric hindrance and lower electrophilicity of the ketones. A dearomatization-rearomatization strategy has been developed for reductive cross-coupling of indoles with ketones in water. Various functional groups and other heterocyclic compounds are tolerated.
Method for preparing N-substituted indole derivative
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Paragraph 0041, (2019/07/01)
The invention discloses a method for preparing a N-substituted indole derivative. The method comprises the steps that under the effect of hydrogen sources and catalytic quantity of palladium system catalysts, indole compounds and ketone used as a hydrocarbylation reagent react; the N-substituted indole derivative is obtained; the indole compound has a structure formula shown in description; the N-substituted indole derivative has a structure formula shown in description, wherein R, R, R, R, R and R are independently nitrogen, alkyl, alkoxy, hydroxy, carboxyl, ester group, aryl, carboxyl alkyl, hydroxyl alkyl and alkoxy alkyl group, or any two adjacent substituent groups in the R, R, R, R, R and R are connected to form 5-6-membered rings; R is selected from a part obtained after oxygen atoms on the carbonyl are removed from the ketone used as the hydrocarbylation reagent. Compared with the prior art, the method has the advantages that the ketone can be used as the hydrocarbylation reagent; the hydrocarbyl or substituted hydrocarbyl is introduced on N bits of the indole; the operation is simpler.
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable stearoyl-CoA desaturase-1 (SCD1) inhibitors: Part 2. Pyridazine-based analogs
Yang, Shyh-Ming,Tang, Yuting,Rano, Thomas,Lu, Huajun,Kuo, Gee-Hong,Gaul, Michael D.,Li, Yaxin,Ho, George,Lang, Wensheng,Conway, James G.,Liang, Yin,Lenhard, James M.,Demarest, Keith T.,Murray, William V.
supporting information, p. 1437 - 1441 (2014/03/21)
Design, synthesis, and biological evaluation of pyridazine-based, 4-bicyclic heteroaryl-piperidine derivatives as potent stearoyl-CoA desaturase-1 (SCD1) inhibitors are described. In a chronic study of selected analog (3e) in Zucker fa/fa (ZF) rat, dose-dependent decrease of body weight gain and plasma fatty acid desaturation index (DI) in both C16 and C18 are also demonstrated. The results indicate that the plasma fatty acid DI may serve as an indicator for direct target engagement and biomarker for SCD1 inhibition.
4-Bicyclic heteroaryl-piperidine derivatives as potent, orally bioavailable Stearoyl-CoA desaturase-1 (SCD1) inhibitors. Part 1: Urea-based analogs
Yang, Shyh-Ming,Tang, Yuting,Zhang, Rui,Lu, Huajun,Kuo, Gee-Hong,Gaul, Michael D.,Li, Yaxin,Ho, George,Conway, James G.,Liang, Yin,Lenhard, James M.,Demarest, Keith T.,Murray, William V.
supporting information, p. 6773 - 6776 (2014/01/06)
A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure-activity relationships focused on bicyclic heteroarenes and aminothiazole-urea portions are discussed. A trend of dose-dependent decrease in body weight gain in diet-induced obese (DIO) mice is also demonstrated.
Strategies for the synthesis of N-(azacycloalkyl)bisindolylmaleimides: Selective inhibitors of PKCβ
Faul, Margaret M.,Grutsch, John L.,Kobierski, Michael E.,Kopach, Michael E.,Krumrich, Christine A.,Staszak, Michael A.,Udodong, Uko,Vicenzi, Jeffrey T.,Sullivan, Kevin A.
, p. 7215 - 7229 (2007/10/03)
N-(Azacycloalkyl)bisindolylmaleimides 1 have been identified to be selective inhibitors of PKCβ. This manuscript will describe the synthetic approaches employed to prepare this class of compounds that resulted in development of efficient methods for prepa
