37921-11-2Relevant academic research and scientific papers
Cyrene as a Bio-Based Solvent for the Suzuki-Miyaura Cross-Coupling
Wilson, Kirsty L.,Murray, Jane,Jamieson, Craig,Watson, Allan J. B.
supporting information, p. 650 - 654 (2017/12/26)
The Suzuki-Miyaura (SM) cross-coupling is the most broadly utilized Pd-catalyzed C-C bond-forming reaction in the chemical industry. A large proportion of SM couplings employ dipolar aprotic solvents; however, current sustainability initiatives and increasingly stringent regulations advocate the use of alternatives that exhibit more desirable properties. Here we describe the scope and utility of the bio-derived solvent Cyrene in SM cross-couplings and evaluate its suitability as a reaction medium for this benchmark transformation from discovery to gram scale.
Stannyl-Lithium: A Facile and Efficient Synthesis Facilitating Further Applications
Wang, Dong-Yu,Wang, Chao,Uchiyama, Masanobu
supporting information, p. 10488 - 10491 (2015/09/28)
We have developed a highly efficient, practical, polycyclic aromatic hydrocarbon (PAH)-catalyzed synthesis of stannyl lithium (Sn-Li), in which the tin resource (stannyl chloride or distannyl) is rapidly and quantitatively transformed into Sn-Li reagent at room temperature without formation of any (toxic) byproducts. The resulting Sn-Li reagent can be stored at ambient temperature for months and shows high reactivity toward various substrates, with quantitative atom efficiency.
Efficient synthesis of 4-substituted pyrazole via microwave-promoted Suzuki cross-coupling reaction
Cheng, Hua,Wu, Qiong-You,Han, Fan,Yang, Guang-Fu
, p. 705 - 709 (2014/06/09)
Pyrazoles and their derivatives are important heterocycles found in nature and present in numerous bioactive compounds. In contrast to 3 or 5-aryl pyrazole, the preparation of 4-aryl pyrazole is fairly rare. Utilizing microwave irradiation, the synthesis of 4-substituted-arylpyrazole via Suzuki cross-coupling has been developed with a wide range of substrates. The remarkable advantages of this method are mild reaction conditions, simple operation, high yield, and short reaction time. Product structures were identified by MS, 1H NMR, 13C NMR, and elemental analysis.
Palladium-catalysed direct diarylations of pyrazoles with aryl bromides: A one step access to 4,5-diarylpyrazoles
Takfaoui, Abdelilah,Zhao, Liqin,Touzani, Rachid,Dixneuf, Pierre H.,Doucet, Henri
, p. 1697 - 1701 (2014/03/21)
The palladium-catalysed direct arylation of pyrazoles with aryl halides, using PdCl(C3H5)(dppb)/KOAc catalyst, reveals a similar reactivity of C4 and C5 CH bonds of pyrazoles, whereas the C3 CH bond is almost unreactive, and gives ac
An improved synthesis of 1-methyl-1H-pyrazole-4-boronic acid pinacol ester and its corresponding lithium hydroxy ate complex: application in Suzuki couplings
Mullens, Peter R.
experimental part, p. 6783 - 6786 (2010/04/27)
An improved synthesis of 1-methyl-1H-pyrazole-4-boronic acid pinacol ester via isolation of the corresponding lithium hydroxy ate complex is described. The hydroxy ate complex is available in one pot from 4-bromo-1-methyl-1H-pyrazole and triisopropyl borate, and is isolated by filtration in high yield. Furthermore, the resulting lithium hydroxy ate complex has long-term bench stability and can be employed directly in Suzuki couplings without the need for added base.
Vasopressin agonist formulation and process
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Page/Page column 50; 51, (2010/02/09)
This invention provides novel formulations for vasopressin agonist compounds, or a pharmaceutically acceptable salt thereof, having the general structure: and processes for making them, the formulations comprising from about 1% to about 20% of active ingredient, from about 1% to about 18% of a surfactant component, from about 50% to about 80% of a component of one or more polyethylene glycols, from about 1% to about 20% of a component of one or more sucrose fatty acid esters and/or polyvinylpyrrolidone and, optionally, one or more preservatives or antioxidants.
Tricyclic vasopressin agonists
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, (2008/06/13)
This invention relates to new compounds selected from those of the general formula (I), or a pharmaceutically acceptable salt, ester or prodrug form thereof: wherein D, E and G are N or CH, which serve as vasopressin agonists and are useful in treating disorders such as diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, and the inability to temporarily delay urination and pharmaceutical compositions and methods for same.
A NEW AND FACILE SYNTHESIS OF 5-ARYLPYRIMIDINES AND 4-ARYLPYRAZOLES
Kano, Shinzo,Yuasa, Yoko,Shibuya, Shiroshi,Hibino, Satoshi
, p. 1079 - 1082 (2007/10/02)
A condensation of 2-aryl-3-(methylthio)acroleins (3a)-(3e), a new masked form of arylmalondialdehydes, with amidines yielded the corresponding 5-arylpyrimidines (4a)-(4k).Similarly, the reaction of 3 with N-substituted hydrazines gave the corresponding 1-
