3882-47-1Relevant academic research and scientific papers
Ruthenium-Catalyzed Direct Asymmetric Reductive Amination of Diaryl and Sterically Hindered Ketones with Ammonium Salts and H2
Hu, Le' an,Zhang, Yao,Zhang, Qing-Wen,Yin, Qin,Zhang, Xumu
supporting information, p. 5321 - 5325 (2020/02/28)
A Ru-catalyzed direct asymmetric reductive amination of ortho-OH-substituted diaryl and sterically hindered ketones with ammonium salts is reported. This method represents a straightforward route toward the synthesis of synthetically useful chiral primary diarylmethylamines and sterically hindered benzylamines (up to 97 % yield, 93–>99 % ee). Elaborations of the chiral amine products into bioactive compounds and a chiral ligand were demonstrated through manipulation of the removable and convertible -OH group.
Natural product inspired library synthesis - Identification of 2,3-diarylbenzofuran and 2,3-dihydrobenzofuran based inhibitors of Chlamydia trachomatis
Saleeb, Michael,Mojica, Sergio,Eriksson, Anna U.,Andersson, C. David,Gylfe, ?sa,Elofsson, Mikael
supporting information, p. 1077 - 1089 (2017/12/15)
A natural product inspired library was synthesized based on 2,3-diarylbenzofuran and 2,3-diaryl-2,3-dihydrobenzofuran scaffolds. The library of forty-eight compounds was prepared by utilizing Pd-catalyzed one-pot multicomponent reactions and ruthenium-catalyzed intramolecular carbenoid C-H insertions. The compounds were evaluated for antibacterial activity in a panel of test systems including phenotypic, biochemical and image-based screening assays. We identified several potent inhibitors that block intracellular replication of pathogenic Chlamydia trachomatis with IC50 ≤ 3 μM. These new C. trachomatis inhibitors can serve as starting points for the development of specific treatments that reduces the global burden of C. trachomatis infections.
Rhodium-Catalyzed Directing-Group-Assisted Aldehydic C–H Arylations with Aryl Halides
Rao, Maddali L. N.,Ramakrishna, Boddu S.
, p. 5080 - 5093 (2017/09/20)
A rhodium-catalyzed general protocol for the directing-group-assisted arylation of aromatic aldehydic C–H bonds was developed. This method involves either hydroxy- or amino-group-directed aldehyde C–H arylation with various aryl halides. A broad synthetic scope for the preparation of 2-hydroxybenzophenones was established with electronically variant salicylaldehydes and aryl halides with chemo- and regioselective possibilities. The developed protocol was also applied in the synthesis of medicinally important 3-salicyloylpyridines in high yields.
Synthesis and evaluation of 3-salicyloylpyridine derivatives as cytotoxic mitochondrial apoptosis inducers
Sood, Alisha,Sharma, Vishal,Chaudhry, Ashun,Kumar, Rakesh,Arora, Saroj,Rajnikant,Gupta, Vivek,Ishar, Mohan Paul S.
supporting information, p. 4724 - 4728 (2015/01/09)
A series of novel 3-salicyloylpyridines (4a-h) were synthesized with good yield by modified Knoevenagel-Stobbel method; o-allylation with allyl bromide lead to formation of compounds (5a-h). The synthesized compounds were characterized by spectroscopic te
Synthesis of some nitrogen heterocycles from the 3-formylchromone-ethyl vinyl ether adduct
Uddin, Rafi,Zaman, Asif
, p. 1039 - 1042 (2007/10/03)
The cyclic acetal grouping and the conjugated double bond of 3-ethoxy-10-oxo-4,4a-dihydro-3H,10H-benzopyranopyran (1a) offer points of attack to nucleophilic reagents.The reaction of 1a with ammonium acetate and hydroxylamine hydrochloride furnish 3-(2'-hydroxybenzoyl)pyridine (3) and its N-oxide 4 with aniline, the amino alcohol 5 and the pyridone 7 and with hydrazine hydrate the diazepin 9.
