scholarly journals An integrated console for capsule-based, automated organic synthesis

2021 ◽  
Author(s):  
Tuo Jiang ◽  
Samuele Bordi ◽  
Angus E. McMillan ◽  
Kuang-Yen Chen ◽  
Fumito Saito ◽  
...  

Using a combination of reagent design, hardware engineering, and a simple operating system we provide an instrument capable of executing complex organic reactions using prepacked capsules with minimal user involvement.

Author(s):  
Tuo Jiang ◽  
Samuele Bordi ◽  
Angus E. McMillan ◽  
Kuang-Yen Chen ◽  
Fumito Saito ◽  
...  

The current laboratory-based practice of organic synthesis renders automation difficult, suffers from safety and environmental hazards, and hampers the implementation of artificial intelligence guided drug discovery. Using a combination of innovative reagent design, hardware engineering, and a simple operating system we provide an instrument capable of executing complex organic reactions with prepacked capsules in a fully automated fashion. The machine conducts coupling reactions and delivers the purified products with minimal user involvement. Two of the most desirable reaction classes – the synthesis of saturated N-heterocycles and reductive amination – were implemented, along with multi-step sequences that provide drug-like organic molecules in a fully automated manner. We envision that this system will serve as a console for developers to provide synthetic methods as integrated, user-friendly packages for conducting organic synthesis in a safe and convenient fashion.


2019 ◽  
Author(s):  
Tuo Jiang ◽  
Samuele Bordi ◽  
Angus E. McMillan ◽  
Kuang-Yen Chen ◽  
Fumito Saito ◽  
...  

The current laboratory-based practice of organic synthesis renders automation difficult, suffers from safety and environmental hazards, and hampers the implementation of artificial intelligence guided drug discovery. Using a combination of innovative reagent design, hardware engineering, and a simple operating system we provide an instrument capable of executing complex organic reactions with prepacked capsules in a fully automated fashion. The machine conducts coupling reactions and delivers the purified products with minimal user involvement. Two of the most desirable reaction classes – the synthesis of saturated N-heterocycles and reductive amination – were implemented, along with multi-step sequences that provide drug-like organic molecules in a fully automated manner. We envision that this system will serve as a console for developers to provide synthetic methods as integrated, user-friendly packages for conducting organic synthesis in a safe and convenient fashion.


Author(s):  
Ghodsi Mohammadi Ziarani ◽  
Fatemeh Mohajer ◽  
Suraj N. Mali

: 1,8-diaminonaphthalene (1,8-DAN) with special organic structure was applied in organic synthesis to provide efficient complex scaffolds, through the two or four-component fashion. This review highlights its recent application in organic reactions under different conditions and heterogynous catalysts to produce various molecules, which were used as medicines, sensors, and dyes.


2021 ◽  
Vol 25 ◽  
Author(s):  
Ghodsi Mohammadi Ziarani ◽  
Fatemeh Javadi ◽  
Fatemeh Mohajer

: The role of oxindole derivatives is discussed as starting materials in diverse organic reactions including two and more components between the years 2014 until 2020. Oxindoles are famous because of their biological properties for instance chromanone-fused polycyclic pyrrolidinyl-dispirooxindoles, functionalized polycyclic spiro-fused carbocyclicoxindole, and 3,3-disubstituted oxindoles have anti-cancer, anti-tumor, and anti-microbial properties, respectively. Therefore, various methods for synthesizing the oxindole structures have received more attention in organic chemistry.


INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (10) ◽  
pp. 24-33
Author(s):  
R. R Somani ◽  
◽  
G. J. Sanap ◽  
P. K Chaskar

In the era of environment friendly chemistry, Microwave Assisted Organic Synthesis (MAOS) has proved to be an effective tool to achieve maximum yield in minimum time without compromising on quality. The present work focuses on synthesis of some bioactive heterocyclic azoles using MAOS. However, the synthetic reactions are optimized using a known technique of factorial designing. Here, 32 factorial design approach is used to achieve the set targets of yields and purity. The outcome has been very promising and opens up new avenues for organic chemists who face challenges in optimizing organic reactions.


2021 ◽  
Vol 25 ◽  
Author(s):  
Saima malik ◽  
Aditya G. Lavekar ◽  
Bimal Krishna Banik

: The radical was first come into existence in 1900 by Gomberg, where the triphenylmethane radical was explored. Thus, even to date, two centuries have seen radical chemistry as the methodology of preference in organic synthesis. Due to the fascinating nature of the radical-mediated cyclization reactions, it always caught the eye of organic chemists for the synthesis of novel organic compounds with diverse stereochemistry. Moreover, the development of radical methods further proves beneficial for the synthesis by providing atom- and step-economical methods to complex molecules. Among these, where radical chemistry has been employed, the use of tin-based radical annulation is the most common and widely used field for the synthesis of a wide range of organic reactions with medicinal importance. In this review, we compiled recent tin-mediated radical cyclization reactions toward the synthesis of molecules of biological significance.


Synlett ◽  
2019 ◽  
Vol 31 (01) ◽  
pp. 21-34 ◽  
Author(s):  
Li Li ◽  
Yun-Long Wei ◽  
Li-Wen Xu

The organosilicon-mediated organic synthesis (SiMOS) has attracted much attention over the recent decades. However, the use of organosilicon reagents with novel catalytic strategies remains to be explored. This Account summarizes our group’s progress mainly based on the application of a wide variety of organosilicon reagents, including allylic silanes, trifluoromethyl silane, acylsilanes, chlorosilanes, hydrosilanes, trimethylsilyldiazomethane, trimethylsiloxyfuran, silanols, α-trimethylsilylmethylacetate, and trimethylsilylcyanide, in catalysis and organic reactions. These transformations were proved to be alternative procedures for the construction of structurally diverse compounds.1 Introduction2 The Exploration of New Reactivity of Organosilicon Reagent in Organic Synthesis2.1 Allylic Silanes2.2 Trifluomethylsilane (TMSCF3)2.3 Acylsilanes2.4 Chlorosilanes and Hydrosilanes2.5 Trimethylsilyldiazomethane (TMSD)2.6 Trimethylsiloxyfuran2.7 Silanols2.8 Trimethylsilylcyanide (TMSCN)3 Conclusion and Perspective


Synthesis ◽  
2020 ◽  
Vol 52 (14) ◽  
pp. 2031-2037
Author(s):  
Antonio Leyva-Pérez ◽  
María Tejeda-Serrano ◽  
Sergio Sanz-Navarro ◽  
Finn Blake

Zeolites are the most used catalysts worldwide in petrochemistry processes, with particular ability to stabilize carbocations. However, the use of zeolites in organic synthesis is still scarce. We show here that representative carboxonium-mediated organic reactions, such as the Nazarov cyclization and the tert-butylation of alcohols with tert-butyl acetate, typically performed with very strong acid catalysts in solution such as triflic acid, can be catalyzed by simple zeolites with high yield and selectivity. The aluminosilicate framework stabilizes the intermediate carboxonium species and overrides the need for superacid protons in solution.


2015 ◽  
Vol 13 (31) ◽  
pp. 8379-8392 ◽  
Author(s):  
Lei Yu ◽  
Mingxuan Liu ◽  
Fenglin Chen ◽  
Qing Xu

The construction of heterocycles from MCPs affords more opportunities for the quick synthesis of elaborately substituted products. This review aims to summarize the novel organic reactions of MCPs to produce heterocycles published in recent years, which have provided specific and powerful tools for organic synthesis.


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