334872-14-9Relevant academic research and scientific papers
Construction of azaspirocyclic skeletons mediated by the carbonyl of the Weinreb amide: Formal total synthesis of (±)-cephalotaxine
Ding, Huili,Fan, Yuxue,Jiang, Minghua,Li, Shanshan,Liu, Jianyin,Liu, Lu,Liu, Tianfu,Zhang, Jian
supporting information, p. 1879 - 1882 (2022/03/15)
A facile Stevens rearrangement of the Weinreb amide and the subsequent key steps mediated by the carbonyl of the Weinreb amide led to the construction of azaspirocyclic skeletons of some typical alkaloids. And the formal total synthesis of (±)-cephalotaxine was completed via a shorter synthetic route by this efficient method. Further studies on the development and asymmetric synthesis application of this strategy are underway. This journal is
PARAZOLE CONDENSED-RING DERIVATIVES AND PREPARATION METHOD THEREOF AND APPLICATION THEREOF IN TREATMENT OF CANCERS, INFLAMMATION AND IMMUNE DISEASES
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Paragraph 0127; 0130, (2018/12/13)
The present invention relates to pyrazole fused-ring derivatives, their preparation methods, and use thereof in medicine. In particular, the present invention relates to a novel derivative represented by formula (I), and a pharmaceutically acceptable salt
NITROGEN RING LINKED DEOXYURIDINE TRIPHOSPHATASE INHIBITORS
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Paragraph 0689, (2018/06/12)
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF
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Paragraph 0271, (2018/12/02)
The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.
COMPOSITIONS AND METHODS COMPRISING SUBSTITUTED 2-AMINOIMIDAZOLES
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Paragraph 0165; 0169, (2018/10/25)
The present invention presents 2-(acylamino)imidazoles with therapeutic activity, including selective activity against cancer cells, and compositions comprising them. Methods of using and preparing the 2-(acylamino)imidazoles are also presented.
Palladium-catalyzed asymmetric allylic alkylation of acyclic ketones for synthesis of 2,2-disubsituted pyrrolidine derivatives
Lian, Wen-Fang,Wang, Cui-Cui,Kang, Huai-Ping,Li, Hai-Ling,Feng, Juan,Liu, Shouxin,Zhang, Zhi-Wei
supporting information, p. 1399 - 1402 (2017/03/17)
Palladium-catalyzed asymmetric allylic alkylation of acyclic ketones represents a significant challenge in organic synthesis. We report herein that the synthesis of chiral 2,2-disubsituted pyrrolidines from acyclic ketones has been accomplished by using catalytic asymmetric method in the presence of Pd(dba)2 and (R)-binap ligand. Theses reactions occur between allyl methyl carbonate and unstabilized acyclic lithium enolates to provide the products in moderate to good enantioselectivity (up to 81% ee).
Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs
Wágner, Gábor,Wéber, Csaba,Nyéki, Olga,Nógrádi, Katalin,Bielik, Attila,Molnár, László,Bobok, Amrita,Horváth, Attila,Kiss, Béla,Kolok, Sándor,Nagy, József,Kurkó, Dalma,Gál, Krisztina,Greiner, István,Szombathelyi, Zsolt,Keser, Gy?rgy M.,Domány, Gy?rgy
scheme or table, p. 3737 - 3741 (2010/08/20)
Here we report the discovery and early SAR of a series of mGluR5 negative allosteric modulators (NAMs). Starting from a moderately active HTS hit we synthesized 3,5-disubstituted-oxadiazoles and tetrazoles as mGluR5 NAMs. Based on the analysis of ligand e
Tetramic acids and derivatives by telluride-triggered dieckmann cyclizations
Dittmer, Donald C.,Avilov, Dmitry V.,Kandula, Venkata Subbarao,Purzycki, Matthew T.,Martens, Zachary J.,Hohn, Elliot B.,Bacler, Matthew W.
experimental part, p. 61 - 83 (2010/09/10)
Treatment of α-bromoacyl amides of esters of N-protected α-amino acids with lithium telluride yields an amide enolate which cyclizes to unstable tetramic acids (2, 4-pyrrolidinediones) which can be converted to stable derivatives (e.g. enol esters, silyl enol ethers, enol tosylates). Reaction conditions are modified to reduce unwanted side reactions: protonation of the enolate, selfcatalyzed intermolecular aldol rections of the tetramic acids, and potential racemization at the α-carbon atom of the amino acid.
Arylation of α-chiral ketones by palladium-catalyzed cross-coupling reactions of tosylhydrazones with aryl halides
Barluenga, Jose,Escribano, Maria,Aznar, Fernando,Valde, Carlos
supporting information; experimental part, p. 6856 - 6859 (2010/12/19)
(Figure Presented) Papa was a rollin' ketone: Arylation of ketones with preservation of the chirality in configurationally unstable α-chiral ketones has been achieved by the palladium-catalyzed cross-coupling reaction between tosylhydrazones and aryl halides (see scheme; Boc=tert-butoxycarbonyl, Ts=4-toluenesulfonyl). The regioselectivity in the β-hydride elimination step is key for the retention of configuration.
Microwave-assisted synthesis of novel (5-nitropyridin-2-yl)alkyl and (5-nitropyridin-3-yl)alkyl carbamates
Henry, Christophe,Haupt, Andreas,Turner, Sean C.
supporting information; experimental part, p. 1932 - 1938 (2009/08/07)
A straightforward approach to novel (5-nitropyridin-2-yl)alkyl and (5-nitropyridin-3-yl)alkyl carbamate building blocks is presented in this study. Their construction is achieved by condensation of N-carbamate a- and β-amino carbonyl derivatives with l-methyl-3,5-dinitro-2-pyridone 1 under microwave irradiation. Judiciously chosen modifications in the nature of the parent carbonyl starting material has influenced the regiochemical outcome of the reaction and allowed an efficient access to novel nitrogen-containing scaffolds. Compounds sharing morphological similarities have been gathered in three libraries differing from each other in a single structural parameter.
