A review on biomass-derived levulinic acid for application in drug synthesis

2021 ◽  
pp. 1-34
Author(s):  
Mingyue Zhang ◽  
Nan Wang ◽  
Jianguo Liu ◽  
Chenguang Wang ◽  
Ying Xu ◽  
...  
Keyword(s):  
Levulinic Acid ◽  
Drug Synthesis

Pd Catalyzed N1/N4 Arylation of Piperazine for Synthesis of Drugs, Biological and Pharmaceutical Targets: An Overview of Buchwald Hartwig Amination Reaction of Piperazine in Drug Synthesis

2018 ◽  
Vol 15 (2) ◽  
pp. 208-220 ◽  
Author(s):  
Vaibhav Mishra ◽  
Tejpal Singh Chundawat
Keyword(s):  
Bond Formation ◽  
Catalyst Design ◽  
Biologically Active ◽  
Reaction Conditions ◽  
Biological Targets ◽  
Amination Reaction ◽  
Drug Synthesis ◽  
Substituted Piperazine ◽  
Approved Drugs ◽  
Fda Approved Drugs

Background: Substituted piperazine heterocycles are among the most significant structural components of pharmaceuticals. N1/N4 substituted piperazine containing drugs and biological targets are ranked 3rd in the top most frequent nitrogen heterocycles in U.S. FDA approved drugs. The high demand of N1/N4 substituted piperazine containing biologically active compounds and U.S. FDA approved drugs, has prompted the development of Pd catalyzed C-N bond formation reactions for their synthesis. Buchwald-Hartwig reaction is the key tool for the synthesis of these compounds. Objective: This review provides strategies for Pd catalyzed C-N bond formation at N1/N4 of piperazine in the synthesis of drugs and biological targets with diverse use of catalyst-ligand system and reaction parameters. Conclusion: It is clear from the review that a vast amount of work has been done in the synthesis of N1/N4 substituted piperazine containing targets under the Pd catalyzed Buchwald-Hartwig amination of aryl halides by using different catalyst-ligand systems. These methods have become increasingly versatile as a result of innovation in catalyst design and improvements in reaction conditions. This review gives an overview of recent utilization of Buchwald-Hartwig amination reaction in drug/target synthesis.

A Novel Scheme for the Synthesis of 21-Acetoxypregna-1,4,9(11)-triene- 17α,21-diol-3,20-dione from 9α-Hydroxyandrostenedione

2020 ◽  
Vol 16 (5) ◽  
pp. 606-610
Author(s):  
Nguyen T. Diep ◽  
Luu D. Huy
Keyword(s):  
Double Bond ◽  
Chemical Synthesis ◽  
Economic Efficiency ◽  
Final Stage ◽  
Side Chain ◽  
Entire Process ◽  
Drug Synthesis ◽  
First Time

Background: Vietnam currently imports up to 90% of the pharmaceuticals it consumes and 100% of the steroid-based pharmaceuticals. The ability for efficient chemical synthesis of the steroids could create commercial opportunities to address this issue. Synthesis of 21-acetoxypregna-1,4,9(11)- triene-17α,21-diol-3,20-dione is considered a key intermediate in the scheme of steroidal drug synthesis. Previous synthesis attempts of such steroids (corticoids) introduce a double bond at C-1(2) in the final stage of synthesis, which delivers a poor yield and reduces the economic efficiency of the process. Objective: To study and develop a novel and effective method for the synthesis of 21-acetoxypregna- 1,4,9(11)-triene-17α,21-diol-3,20-dione. Methods: Using 9α-hydroxyandrostenedione as a substrate chemical synthesis was performed as follows: pregnane side chain construction at C-17 (acetylene method), introduction of C-1(2) double bond (using SeO2), epimerization of C-17 (via 17-ONO2 ester) and Stork’s iodination. Results: 21-acetoxypregna-1,4,9(11)-triene-17α,21-diol-3,20-dione was prepared from 9α- hydroxyandrostenedione with an improved yield compared to previous attempts. Conclusion: Here, 21-acetoxypregna-1,4,9(11)-triene-17α,21-diol-3,20-dione has been synthesized from 9α-hydroxyandrostenedione based on a novel, effective and commercially feasible scheme. The introduction of the C-1(2) double bond at an earlier stage of the synthesis has increased the economic efficiency of the entire process. For the first time, the indirect epimerization mechanism has been clarified along with the configuration of the C-17 stereo-center which has been confirmed using NOESY data.

Nyctanthes Arbor-Tristis and its Role in the Alleviation of Arthritic Pain: A Review

2020 ◽  
Vol 16 (8) ◽  
pp. 1147-1156
Author(s):  
Ruchi Singh ◽  
Syed M. Hasan ◽  
Amit Verma ◽  
Sanjay K. Panda
Keyword(s):  
Research Work ◽  
Plant Distribution ◽  
Pharmacological Activities ◽  
Whole Plant ◽  
Modern Drug ◽  
Active Chemical ◽  
Drug Synthesis ◽  
New Compounds

Background: A plant is a reservoir of potentially useful active chemical entities which act as drugs as well as intermediates for the discovery of newer molecules and provide newer leads for modern drug synthesis. The demand for new compounds in the field of medicine and biotechnology is centuries old and with a rise in chronic diseases and resistance to existing drugs in the field of anti-infective agents, the chemicals obtained from plant sources have been an area of attraction. The whole plant has possessed multiple pharmacological activities. This is scientifically established by in-vivo and in-vitro studies. Methods: Various electronic databases such as PubMed, Science Direct, Scopus and Google were searched to collect the data of the present review. All the collected information is categorized into different sections as per the aim of the paper. Results: Fifty-six research and review papers have been studied and were included in this review article. After a detailed study, we provide a significant description of various phytochemicals present in Nyctanthes arbor-tristis Linn., which is responsible for various pharmacological activities. Twenty of studied articles gives a general introduction and ethnobotanical information about the plant, two papers contained microscopic detail of leaf and fruit. Twenty papers contained information about the phytoconstituents present in different parts of Nyctanthes arbor-tristis plant and fourteen articles reported pharmacological activities like antioxidant, anti-inflammatory, antiarthritic, antimicrobial and immunobiotic activity. Conclusion: This review explores the published research work comprising the ethnobotanical description of the subjected plant, distribution, phytochemical profile, and arthritis-related pharmacological activities.

Photodynamic Therapy of Normal and Balloon-Injured Rat Carotid Arteries Using 5-Amino-Levulinic Acid

Circulation ◽  
1995 ◽  
Vol 91 (2) ◽  
pp. 417-425 ◽  
Author(s):  
Isaac Nyamekye ◽  
Sandra Anglin ◽  
Jean McEwan ◽  
Alexander MacRobert ◽  
Stephen Bown ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Levulinic Acid ◽  
Carotid Arteries ◽  
Amino Levulinic Acid

Mono- and bimetallic (Ru-Co) polymeric catalysts for levulinic acid hydrogenation

2020 ◽  
Author(s):  
Maxim E. Grigorev ◽  
Stepan P. Mikhailov ◽  
Alexey V. Bykov ◽  
Alexander I. Sidorov ◽  
Irina Yu. Tiamina ◽  
...  
Keyword(s):  
Levulinic Acid

Chiral imidazolidinones: A class of priviliged organocatalysts in stereoselective organic synthesis

2020 ◽  
Vol 5 (5) ◽  
Author(s):  
Laura Raimondi ◽  
Chiara Faverio ◽  
Monica Fiorenza Boselli
Keyword(s):  
Pharmaceutical Industry ◽  
Green Chemistry ◽  
Organic Synthesis ◽  
Catalytic Synthesis ◽  
Biological Chemistry ◽  
Chiral Molecules ◽  
Catalytic Systems ◽  
Drug Synthesis ◽  
Industry Needs

AbstractChiral molecules hold a mail position in Organic and Biological Chemistry, so pharmaceutical industry needs suitable strategies for drug synthesis. Moreover, Green Chemistry procedures are increasingly required in order to avoid environment deterioration. Catalytic synthesis, in particular organocatalysis, in thus a continuously expanding field. A survey of more recent researches involving chiral imidazolidinones is here presented, with a particular focus on immobilized catalytic systems.

Selective conversion of furfuryl alcohol to levulinic acid by SO3H-containing silica nanoflower in GVL/H2O system

2021 ◽  
Vol 171 ◽  
pp. 124-132
Author(s):  
Ruoqing Wang ◽  
Feng Shen ◽  
Yiwei Tang ◽  
Haixin Guo ◽  
Richard Lee Smith ◽  
...  
Keyword(s):  
Furfuryl Alcohol ◽  
Levulinic Acid ◽  
Selective Conversion

scholarly journals Mini-Review on the Synthesis of Furfural and Levulinic Acid from Lignocellulosic Biomass

Processes ◽  
2021 ◽  
Vol 9 (7) ◽  
pp. 1234
Author(s):  
Zhiwei Jiang ◽  
Di Hu ◽  
Zhiyue Zhao ◽  
Zixiao Yi ◽  
Zuo Chen ◽  
...  
Keyword(s):  
Reaction Mechanism ◽  
Lignocellulosic Biomass ◽  
Catalytic System ◽  
Levulinic Acid ◽  
Value Added ◽  
Environmental Issues ◽  
Alternative Route ◽  
Catalytic Systems ◽  
Renewable Biomass ◽  
Platform Chemicals

Efficient conversion of renewable biomass into value-added chemicals and biofuels is regarded as an alternative route to reduce our high dependence on fossil resources and the associated environmental issues. In this context, biomass-based furfural and levulinic acid (LA) platform chemicals are frequently utilized to synthesize various valuable chemicals and biofuels. In this review, the reaction mechanism and catalytic system developed for the generation of furfural and levulinic acid are summarized and compared. Special efforts are focused on the different catalytic systems for the synthesis of furfural and levulinic acid. The corresponding challenges and outlooks are also observed.

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