24654-09-9Relevant academic research and scientific papers
Consecutive Three-Component Coupling-Addition Synthesis of β-Amino Enoates and 3-Hydroxypyrazoles via Ethyl 3-Arylpropiolates
Niedballa, Jonas,Reiss, Guido J.,Müller, Thomas J. J.
supporting information, p. 5019 - 5024 (2020/07/24)
Two consecutive three-component syntheses furnishing β-amino enoates or 3-hydroxypyrazoles based upon the Sonogashira alkynylation of aryl iodides and ethyl propiolate were established in mostly excellent yields. The ethyl 3-arylpropiolate intermediates are Michael systems which are suited for concatenation with conjugate addition or cyclocondensation giving access to libraries of 21 different β-amino enoates and 17 different 3-hydroxypyrazoles. The rotational barrier of β-pyrrolidino enoates was assessed by studying the coalescence of pyrrolidinyl protons in VT-NMR spectra of electronically different substituted derivatives showing that the electronic substituent effect on the aryl group does not affect the height of the rotational barrier. This indicates that the substituents are essentially oriented orthogonally to the plane of the β-pyrrolidino enoates.
Synthesis of novel benzochromenes using triarylphosphines, alkyl X-phenylpropiolates and 2-hydroxy-1-naphthaldehyde
Gholami, Hamid Reza,Asghari, Sakineh
, p. 206 - 209 (2018/05/26)
The reactions of a series of alkyl X-phenylpropiolates with 2-hydroxy-1-naphthaldehyde and triphenylphosphine led to benzochromenes in moderate yields. When the reactions were performed in the presence of bis(4-methoxyphenyl)phenylphosphine instead of tri
Gold-catalyzed Fluorination of Alkynyl Esters and Ketones: Efficient Access to Fluorinated 1,3-Dicarbonyl Compounds
Zeng, Xiaojun,Lu, Zhichao,Liu, Shiwen,Hammond, Gerald B.,Xu, Bo
supporting information, p. 4062 - 4066 (2017/11/30)
We developed an efficient synthesis of 2-fluoro-1,3-dicarbonyl compounds using readily available alkynyl ketones or esters as starting material. The key step is the insertion of hydrogen fluoride (HF) to the gold carbene intermediate generated from cationic gold catalyzed addition of N-oxides to alkynyl ketones or esters. This method gives excellent chemical yields and regioselectivity with good functional group tolerance. (Figure presented.).
MODULATORS OF CASPASE-6
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Paragraph 000109, (2016/04/26)
The current application relates to a pharmaceutical composition for the treatment or amelioration of a neurological disease, wherein the composition comprises a therapeutically effective amount of a caspase-6 inhibitor which is an arylpropynamide derivative. The composition can be formulated for oral or topical administration, subcutaneous, intravenous, or intramuscular injection, infusion, inhalation, or intrthecal injection.
Structural design and synthesis of arylalkynyl amide-type peroxisome proliferator-activated receptor γ3 (PPAR γ3)-selective antagonists based on the helix12-folding inhibition hypothesis
Ohashi, Masao,Gamo, Kanae,Tanaka, Yuta,Waki, Minoru,Beniyama, Yoko,Matsuno, Kenji,Wada, Jun,Tenta, Masafumi,Eguchi, Jun,Makishima, Makoto,Matsuura, Nobuyasu,Oyama, Takuji,Miyachi, Hiroyuki
, p. 53 - 67 (2015/01/08)
Peroxisome proliferator-activated receptor γ3 (PPARγ3) antagonists are candidates for treatment of type 2 diabetes, obesity and osteoporosis. However, few rational design strategies are currently available. Here, we utilized the helix12 (H12)-folding inhi
Preparation of arylpropynamides and their reaction with malonyl acid derivatives
Petina, Olgaa. A.,Yakovlev, Igorp. P.,Geffken, Detlef
, p. 803 - 809 (2013/04/10)
Synthesis of arylpropynamides and their reactions with different malonic acid derivatives is described. Treatment of arylpropynamides with unsubstituted malonyl chloride furnished N-(3-arylprop-2-ynoyl)-6-chloro-4-hydroxy-2-oxo-2H- pyran-3-carboxamides; m
The reaction of substituted ethyl α-bromocinnamates with tetrabutyl ammonium fluoride
Liang, Yan,Zhang, Ying Peng,Yu, Wei
experimental part, p. 777 - 780 (2012/08/27)
The reaction of ethyl α-bromocinnamates with tetrabutyl ammonium fluoride (TBAF) was influenced largely by the position of the substituent at the phenyl ring. While the substrates without an ortho substituent at the phenyl ring were transformed to the cor
Preparation of α-bromoacrylates: One-pot procedure for the synthesis of conjugated acetylenic carboxylates from aldehydes with Ph3P/ Br3CCO2Et
Kim, Joong-Gon,Dong, Ho Kang,Doo, Ok Jang
, p. 443 - 447 (2008/04/01)
We have established the optimal conditions for the Wittig reaction for synthesizing α-bromoacrylates with a high selectivity, and developed a simple and efficient one-pot procedure for preparing various conjugated acetylenic carboxylates in moderate to high yields. Georg Thieme Verlag Stuttgart.
TACHYKININ RECEPTOR ANTAGONISTS
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Page 26-27, (2010/02/10)
The present invention relates to selective NK-1 receptor antagonists of Formula (I) or a pharmaceutically acceptable salt thereof, for the treatment of disorders associated with an excess of tachykinins.
Diaryl-enynes
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, (2008/06/13)
Provided, among other things, is a compound of Formula I: wherein: Ar1and Ar2are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkox
