131529-87-8Relevant academic research and scientific papers
Ruthenium/chloride catalytic system for conjugate addition of terminal alkynes to acrylate esters
Nishimura, Takahiro,Washitake, Yosuke,Nishiguchi, Yoshiki,Maeda, Yasunari,Uemura, Sakae
, p. 1312 - 1313 (2004)
The addition of terminal alkynes to acrylate esters in the presence of a ruthenium catalyst and chloride sources proceeds to give the corresponding γ,δ-alkynyl esters in good yields.
Copper(II)-Mediated Ring Opening/Alkynylation of Tertiary Cyclopropanols by Using Nonmodified Terminal Alkynes
Cheng, Bu-Qing,Zhang, Si-Xuan,Cui, Yan-Ying,Chu, Xue-Qiang,Rao, Weidong,Xu, Haiyan,Han, Guo-Zhi,Shen, Zhi-Liang
supporting information, p. 5456 - 5461 (2020/07/14)
The copper(II)-mediated ring opening/alkynylation of cyclopropanol by employing inexpensive and commercially available terminal alkyne is developed. The reactions proceeded efficiently to afford synthetically useful alk-4-yn-1-ones in moderate to good yie
Method for preparing 4-acetylenic ketone/ester compound and application thereof
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Paragraph 0064-0077, (2020/06/20)
The invention relates to a method for preparing a 4-acetylenic ketone/ester compound and an application thereof, and particularly provides a preparation method of a copper-mediated 4-acetylenic ketone/ester compound. The process is mild in reaction conditions and good in yield, and the compound has strong functional group tolerance and good compatibility.
Rapid Access to Thiolactone Derivatives through Radical-Mediated Acyl Thiol-Ene and Acyl Thiol-Yne Cyclization
McCourt, Ruairi O.,Dénès, Fabrice,Sanchez-Sanz, Goar,Scanlan, Eoin M.
supporting information, p. 2948 - 2951 (2018/05/28)
A new synthetic approach to thiolactones that employs an efficient acyl thiol-ene (ATE) or acyl thiol-yne (ATY) cyclization to convert unsaturated thiocarboxylic acid derivatives into thiolactones under very mild conditions is described. The high overall yields, fast kinetics, high diastereoselectivity, excellent regiocontrol, and broad substrate scope of these reaction processes render this a very useful approach for diversity-oriented synthesis and drug discovery efforts. A detailed computational rationale is provided for the observed regiocontrol.
LACTAM COMPOUNDS AS EP4 RECEPTOR-SELECTIVE AGONISTS FOR USE IN THE TREATMENT OF EP4-MEDIATED DISEASES AND CONDITIONS
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Paragraph 0453; 0460; 0461, (2014/09/29)
Disclosed herein are compounds of formula (I) wherein L1, L2, L3, R1, R4, R5, and R6 are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, osteoporosis, bone fracture, periodontal bone loss, orthopedic implant, alopecia, neuropathic pain, and related disorders. Pharmaceutical compositions and methods of treating conditions or disorders are also described.
Direct conjugate addition of alkynes with α,β-unsaturated carbonyl compounds catalyzed by NCN-pincer Ru complexes
Ito, Jun-Ichi,Fujii, Kohei,Nishiyama, Hisao
supporting information, p. 601 - 605 (2013/03/13)
NCN-pincer Ru-complexes containing bis(oxazolinyl)phenyl ligands serve as suitable catalysts in the direct conjugate additions of α,β- unsaturated carbonyl compounds, including ketones, esters, and amides, as well as vinylphosphonates, giving various β-alkynyl carbonyl and phosphonate compounds. A bis(oxazolinyl)phenyl (phebox)-Ru complex also catalyzes the asymmetric conjugate addition of an alkyne with a β-substituted, α,β-unsaturated ketone to produce a chiral β-alkynyl ketone. Copyright
Indium(III) chloride catalyzed conjugate addition reaction of alkynylsilanes to acrylate esters
Xu, Yan-Li,Pan, Ying-Ming,Liu, Pei,Wang, Heng-Shan,Tian, Xiao-Yan,Su, Gui-Fa
experimental part, p. 3557 - 3562 (2012/05/31)
A novel and efficient procedure for the synthesis of δ,γ- alkynyl esters by the conjugate addition of alkynylsilanes to acrylate esters in the presence of a catalytic amount of indium(III) chloride has been developed. This method provides a rapid and efficient access to substituted δ,γ-alkynyl esters.
Alkyne-mediated domino hydroformylation/double cyclization: Mechanistic insight and synthesis of (±)-tashiromine
Chiou, Wen-Hua,Lin, Yi-Huei,Chen, Guei-Tang,Gao, Yu-Kai,Tseng, Yu-Che,Kao, Chien-Lun,Tsai, Jui-Chi
supporting information; experimental part, p. 3562 - 3564 (2011/04/26)
A novel domino reaction, alkyne-mediated domino hydroformylation/double cyclization, has been developed for rapid preparation of indolizidine type alkaloids. DFT calculations were applied for rationales of reactivity and selectivity. A concise synthesis of tashiromine as the application of the methodology is also reported.
An effective synthetic entry to fused benzimidazoles via iodocyclization
Zhang, Xu,Zhou, Yu,Wang, Hengshuai,Guo, Diliang,Ye, Deju,Xu, Yungen,Jiang, Hualiang,Liu, Hong
supporting information; experimental part, p. 1429 - 1437 (2011/08/03)
A protocol for the synthesis of the fused heterocyclic polycyclic compounds pyrrole[1,2-a]benzimidazoles, piperidine[1,2-a]benzimidazoles and oxa-fused benzimidazoles using iodine and silver nitrate by an exo-dig or endo-dig cyclization pathway at room te
Intramolecular PIFA-mediated alkyne amidation and carboxylation reaction
Tellitu, Imanol,Serna, Sonia,Herrero, M. Teresa,Moreno, Isabel,Dominguez, Esther,SanMartin, Raul
, p. 1526 - 1529 (2007/10/03)
(Chemical Equation Presented) The hypervalent iodine reagent PIFA promotes the intramolecular electrophilic cyclization of easily accessible alkynylamides and alkynyl carboxylic acids, leading to the formation of pyrrolidinone and lactone skeletons, respe
