scholarly journals Structural diversification of the aminobicyclo[4.3.0]nonane skeleton using alkynylsilyl-derived allylic trichloroacetimidates

2017 ◽  
Vol 15 (14) ◽  
pp. 3035-3045 ◽  
Author(s):  
Mohamed A. B. Mostafa ◽  
Angus E. McMillan ◽  
Andrew Sutherland

The late-stage synthesis of aminobicyclo[4.3.0]nonane analogues has been achieved from a key vinylsilane intermediate, prepared in turn by a one-pot multi-step process using an alkynylsilyl-derived allylic trichloroacetimidate.

2019 ◽  
Vol 17 (18) ◽  
pp. 4629-4639 ◽  
Author(s):  
Martyn C. Henry ◽  
Rochelle McGrory ◽  
Réka J. Faggyas ◽  
Mohamed A. B. Mostafa ◽  
Andrew Sutherland

A one-pot ortho-amination of activated arenes using sequential iron and copper catalysis has been developed and utilised for the late-stage structural diversification of biologically active 3,4-dihydroquinolin-2-ones.


2019 ◽  
Author(s):  
Victor Bloemendal ◽  
Floris P. J. T. Rutjes ◽  
Thomas J. Boltje ◽  
Daan Sondag ◽  
Hidde Elferink ◽  
...  

<p>In this manuscript we describe a modular pathway to synthesize biologically relevant (–)-<i>trans</i>-Δ<sup>8</sup>-THC derivatives, which can be used to modulate the pharmacologically important CB<sub>1</sub> and CB<sub>2</sub> receptors. This pathway involves a one-pot Friedel-Crafts alkylation/cyclization protocol, followed by Suzuki-Miyaura cross-coupling reactions and gives rise to a series of new Δ<sup>8</sup>-THC derivatives. In addition, we demonstrate using extensive NMR evidence that similar halide-substituted Friedel-Crafts alkylation/cyclization products in previous articles were wrongly assigned as the para-isomers, which also has consequence for the assignment of the subsequent cross-coupled products and interpretation of their biological activity. </p> <p>Considering the importance of the availability of THC derivatives in medicinal chemistry research and the fact that previously synthesized compounds were wrongly assigned, we feel this research is describing a straightforward pathway into new cannabinoids.</p>


2020 ◽  
Vol 977 ◽  
pp. 102-107
Author(s):  
Yu Lei Zheng ◽  
Shuang Chen ◽  
Jia Hui Wang ◽  
Ru Xiao

Polyamide 66 (PA66) benefits from excellent mechanical properties and good chemical resistance, which enabled wide application of this material in various industrial fields; however, it suffers from high flammability. Generally, preparation of a flame retardant PA from a reactive flame retardant involves a two-step process. In this study, the flame retardant PA66s (FRPA66s) are synthesized via a one-pot melt copolycondensation route by using a reactive phosphorus-containing flame retardant (FR-B). Then, molecular weight, some mechanical and thermal properties along with flame retardant properties of FRPA66s were investigated by gel permeation chromatography (GPC), instron material testing, differential scanning calorimetry (DSC), thermogravimetry (TG) analysis, vertical burning test (UL 94), and limiting oxygen index test (LOI) techniques. The experimental results confirmed that FRPA66s synthesized by the one-pot method have very similar properties compared to those obtained via the two-step process. Moreover, the prepared materials showed good non-flammability behavior with limiting oxygen index value of over 30% and a vertical burning test result of V-0 rating.


2018 ◽  
Vol 24 (40) ◽  
pp. 10186-10195 ◽  
Author(s):  
Irene Hernández Delgado ◽  
Simon Pascal ◽  
Céline Besnard ◽  
Silvia Voci ◽  
Laurent Bouffier ◽  
...  

RSC Advances ◽  
2016 ◽  
Vol 6 (4) ◽  
pp. 3301-3306 ◽  
Author(s):  
Ibtissam Bassoude ◽  
Zahira Tber ◽  
El Mokhtar Essassi ◽  
Gérald Guillaumet ◽  
Sabine Berteina-Raboin

An efficient synthesis of 7-substituted pyrazolo[1,5-a]pyrimidines using a one-pot, two-step process via Pd-catalyzed direct CH-arylation followed by a saponification–decarboxylation reaction is reported.


2013 ◽  
Vol 9 ◽  
pp. 2378-2386 ◽  
Author(s):  
Diego Carnaroglio ◽  
Katia Martina ◽  
Giovanni Palmisano ◽  
Andrea Penoni ◽  
Claudia Domini ◽  
...  

A fast and efficient protocol for the synthesis of N,N'-disubstituted urea derivatives from alkyl halides and primary or secondary amines has been developed. The synthetic pathway combines nucleophilic substitutions and a Staudinger–aza-Wittig reaction in the presence of polymer-bound diphenylphosphine under 14 bar of CO2 pressure and has been performed in a one-pot two-step process. The protocol has been optimized under microwave irradiation and the scale-up experiment has been conducted under conventional conditions in a Parr reactor. The final compounds were isolated after simple filtration in almost quantitative overall yields which makes this procedure facile and rapid to execute.


2020 ◽  
Vol 20 (10) ◽  
pp. 6286-6294
Author(s):  
Mukerem Helil Abib ◽  
Taotao Chen ◽  
Enze Xu ◽  
Man Wang ◽  
Yang Jiang

Environmentally friendly and long PL lifespan Mn-doped CuInZnS (Mn:CIZS) and CuInZnS/ZnS (Mn:CIZS/ZnS) QDs, with respective red and yellow emissions, were synthesized using nontoxic precursors via a facile dual-step process based on the one-pot method. The resulting Mn:CIZS and Mn:CIZS/ZnS QDs exhibited confirmed strong red and yellow photoluminescence emissions at approximately 654 nm and 580 nm, respectively. The measured PL decay lifespan for the Mn: CIZS QDs is 2.52 μs due to well-organized surface passivation through the ZnS shell; the average PL lifespan for the Mn:CIZS/ZnS QDs is extended to 6.28 μs. Moreover, the WLEDs were composed of the Mn:CIZS/ZnS QDs. The resulting WLEDs offered admirable optical attributes, such as an excellent Ra of 89, a low Tc of 5075 K and radiant white light emanation at 60 mA functional current. Therefore, the outputs highlight the Mn:CIZS/ZnS QDs as hopeful cadmium-free resources for the interest of optoelectronics exploration.


2016 ◽  
Vol 523 ◽  
pp. 73-84 ◽  
Author(s):  
Alejandro Prieto ◽  
Miguel Palomino ◽  
Urbano Díaz ◽  
Avelino Corma

2011 ◽  
Vol 9 (8) ◽  
pp. 2821 ◽  
Author(s):  
Jolanta Hałuszczak ◽  
Simon J. F. Macdonald ◽  
Marie E. Migaud
Keyword(s):  
One Pot ◽  

2016 ◽  
Vol 14 (12) ◽  
pp. 3284-3297 ◽  
Author(s):  
Mohamed A. B. Mostafa ◽  
Mark. W. Grafton ◽  
Claire Wilson ◽  
Andrew Sutherland

A one-pot multi-step process that uses both Pd(ii)- and Ru(ii)-catalysis has been developed for the diastereoselective synthesis of aminobicyclo[4.3.0]nonanes.


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