Amir Moqaddari’s Post

A very nice presentation of relationship between total synthesis vs medicinal chemistry.

The best types of training in academia for practicing modern medicinal chemistry in the pharmaceutical and biotechnology industries of today. In this viewpoint article 'Total Synthesis as Training for Medicinal Chemistry', the case is made for the ongoing, and perhaps increasing, value of total synthesis as training for medicinal chemistry. A must-read for anyone passionate about the future of medicinal chemistry. #MedicinalChemistry #TotalSynthesis #PharmaceuticalIndustry"

https://lnkd.in/g8-yhQCk Total synthesis training helps building medicinal chemistry acumen.

Excellent read, Lew. Thank you for putting your perspectives out there. My experience is that the skills from total synthesis also translated to the design and synthesis of "small" molecules for organic electronics applications. Our lab has done "med-chem" type work there, but with different parameters on the deliverable (solid state or crystal packing, band-gap, solubility, etc, etc). These projects also required a similar optimization cycle as you discussed in the paper. A potential difference being that we typically needed to deliver 100mg-5g quantities of pure material (passed combustion analysis). I'm teaching "Advanced Organic" to our chemistry and medicinal chemistry graduate students next semester at the University of Minnesota. This year I'm considering making the capstone project for the course a natural product synthesis proposal. With a fairly large enrollment (~30), if any total synthesis enthusiasts are willing to serve - either as a proposal judge or a mentor - please ping me. I plan to have your paper as (hopefully) inspirational reading for the students. Cheers.

Total Synthesis as Training for Medicinal Chemistry. Ingo Hartung wrote a fantastic discussion on this topic on Twitter. Here is the link: 👉 https://lnkd.in/euBXUeUn The summary is here: 👇 While total synthesis is a valuable training ground for medicinal chemists, its over-competitive culture has stifled innovation. It emphasizes the importance of a holistic understanding of reactivity, problem-solving skills, and a translational mindset in medicinal chemistry. However, there is a lack of collaboration in traditional total synthesis groups and innovation in the chemical biology community. It suggests that graduates with a pure total synthesis background sometimes face competition, but those with a collaborative mindset and willingness to branch out have promising opportunities ahead. #totalsynthesis #organicchemistry #medicinalchemistry #chemicalbiology #drugdiscovery #drugdevelopment

Medicinal chemistry is one of the interesting subjects in medicinal science. Medicinal Chemistry ▷ Antibiotics Penicillin It developed since 1930s Most common Antibiotics drug Most popular Great mechanism of action

Palladium chemistry is frequently used in the synthesis of Active Pharmaceutical Ingredients (APIs) due to its versatility in forming complex carbon-carbon and carbon-heteroatom bonds. Some common applications of palladium chemistry in API synthesis include: 1. Cross-coupling reactions: Palladium-catalyzed cross-coupling reactions are used to construct key structural motifs in many pharmaceutical compounds. For example, the Suzuki-Miyaura coupling is widely employed for the synthesis of biaryl compounds found in numerous drugs. 2. Hydrogenation reactions: Palladium-catalyzed hydrogenation is used to reduce unsaturated bonds in molecules, allowing for the synthesis of saturated compounds or the selective reduction of functional groups. 3. Carbonylation reactions: Palladium-catalyzed carbonylation reactions are used to introduce carbonyl groups into organic molecules, enabling the synthesis of aldehydes, ketones, esters, and other carbonyl-containing compounds. Handling palladium chemistry in API synthesis requires adherence to strict safety protocols due to the potential toxicity of palladium compounds and the high reactivity of some palladium catalysts. Key considerations include: - Proper training: Personnel involved in handling palladium chemistry should receive adequate training in safe laboratory practices, including handling of air-sensitive reagents, use of appropriate protective equipment, and waste disposal procedures. - Controlled environment: Palladium-catalyzed reactions are often conducted under inert atmospheres (e.g., nitrogen or argon) to minimize the risk of oxidation and ensure the stability of palladium catalysts. - Monitoring and control: Reaction parameters such as temperature, pressure, and catalyst loading should be carefully monitored and controlled to optimize reaction efficiency and minimize the formation of unwanted by-products. - Waste management: Proper disposal of reaction by-products and spent catalysts is essential to minimize environmental impact and ensure compliance with regulatory requirements. Palladium chemistry in API synthesis can be used in various stages of drug development, including: - Medicinal chemistry: Palladium-catalyzed reactions are employed in the synthesis of novel drug candidates during the medicinal chemistry optimization phase. - Process development: Palladium chemistry is used to develop scalable and cost-effective synthetic routes for API production. #reactions #reactions #mechanisms #mechanism #chemistryclass #chemistry #chemistrylove #chemistry2 #chemistrymemes #chemistrynotes #chemistryexperiments #chemistryisfun #chemistryeducation #chemistrystudent #chemistrylab #chemistrylovers #chemistrycafe #chemistrymajor #sciencerules #scientists #science #scienceworld #chemistrymeme #chemistrylovers #chemistryteacher #chemistryteachers #chemistryisfun #chemistry2 #chemistryexperiments #chemistrynotes #chemistrystudent #pharmaceuticals #pharmaceutical #qualityassurance #qualitycontrol

Check out the latest issue of Acta Chemica and Pharmaceutica for cutting-edge research in chemistry and pharmacy! 📚💊 Don't miss out on exciting discoveries and advancements in the field. #Chemistry #Pharmacy #Research #Science

What is Docking in Modern Medicinal Chemistry and Drug Discovery?

Creative Design in Chemistry   In medicinal chemistry, the difference of one atom in a compound can have an impact on the bonding and stability which can affect drug effectiveness. One of the most common modifications done to drugs is the changing of an aromatic carbon to a nitrogen atom. The prevalence of having this nitrogen has resulted in the idea of having a “necessary nitrogen atom” for effective drug design. The problem with this method is that the changing of a single atom in practice is indirect and a restart of synthesis needs to happen to produce the desired change.   However, a paper1 published at the end of 2023, suggests a direct transformation done via oxidative restructuring with ozone gas. This reaction forms a ring-opened intermediate which is electrophilic and allows for the reaction that will result in the release of a carbon atom and reforming of the ring. This method allows for more accurate modification due to the less effect it has on the compound's skeleton-rotation which is an often-seen pitfall in the synthesis of a modified drug. This process of analysis and modification is something that I have had to do during my time at the University of Newcastle. During the completion of a Medicinal and Biological chemistry, from given structures and biological test results I was asked about how to improve drug effectiveness. Using my knowledge and critical thinking, I suggested ways in which modifications could be used to improve the drugs activity as well as provide a synthesis for the suggestions. I received a 80% grade for my answers towards these questions. #SCIE2001 #BScUoN (1)    Woo, J.; Stein, C.; Christian, A. H.; Levin, M. D. Carbon-To-Nitrogen Single-Atom Transmutation of Azaarenes. Nature 2023, 623 (7985), 77–82. https://lnkd.in/e5WijiH2 Pixabay, https://lnkd.in/e3jXdkWE , (Creative Commons licenced).