Synthetic Development of Key Intermediates and Active Pharmaceutical Ingredients DOI
Luca Laraia, Nilanjana Majumdar, Gangarajula Sudhakar

и другие.

Опубликована: Май 29, 2024

The development of efficient and sustainable synthetic processes for pharmaceuticals is a critical area research, primarily driven by the pharmaceutical industry. However, fostering such research in academic institutions holds immense potential. SYNTHESIS special issue on "Synthetic Development Key Intermediates Active Pharmaceutical Ingredients (APIs)" highlighted recent advancements this field. In Thieme Cheminar chaired Prof. Laha (Guest Editor “Synthetic (APIs)” collection) our speakers will share discuss their results Chair: * Joydev Kumar (National Institute Education Research, India) Our speakers: Dr. Luca Laraia (Technical University Denmark): Next-generation strategies synthesis functional, natural product inspired compounds. Sharada Prasanna Swain Research): Photocatalyzed Continuous-flow Pharmaceuticals. Gangarajula Sudhakar (CSIR- Indian Chemical Technology): role steps order developing key intermediates active ingredients. Nilanjana Majumdar (CSIR-Central Drug Research Institute): Unactivated Carboxylic Acids Catalytic Asymmetric Ring Opening Reactions. compounds Natural products derivatives have been source bioactive therapeutics centuries; however, isolation feasibility challenges hamper use. Chemists sought to address rapidly access larger numbers product-inspired compounds, including diversity- biology-oriented (DOS BIOS), complexity-to-diversity (CtD) pseudo-natural (PNPs). lecture I highlight group’s work combining all above specific biological challenges, selective inhibitors sterol transport proteins (STPs) G-protein coupled receptors (GPCRs), as well new photochemical methods diverse scaffolds from cheap, abundant products. Reactions acids are considered feedstock chemicals they widely available, highly stable inexpensive. They can be excellent choice substrates catalytic asymmetric reactions but quite challenging well. Free carboxylic generally not compatible various transformations, e.g. difficult nucleophilic or electrophilic reactions. Here, convenient use free acid illustrated ring opening preparation important class that may act useful chiral synthons. ingredients tailored target requirements often differs significantly between process chemistry. chemistry, emphasis typically using known, reliable, readily available raw materials ensure commercial viability, rather than employing complex specialized reagents. A consistent focus large-scale manufacturing involves avoiding costly hazardous reagents reaction conditions, enhancing yields, reducing waste generation. some instances, minor modifications yield significant benefits, improved environmental impact, cost reduction, more materials, increased energy efficiency step economy. line with these objectives, has led novel route an advanced intermediate Ledipasvir. This late-stage cyclopropanation fluorination. Additionally, we devised telescopic Gliflozin Aglycone, which includes ortho-lithiation 1,4-dihalobenzene followed corresponding aldehydes subsequent reduction resulting diaryl methanol intermediate. These innovative laboratory-scale syntheses currently being evaluated potential scale-up processes, reflecting commitment optimizing through strategic, incremental improvements. Pharmaceuticals Flow chemistry helps safe handling reagents, high temp. reactions, scalable photocatalyzed Boron containing building blocks Suzuki coupling drug molecules Tavaborole, (antifungal), Crisaborole Bortezomib (anticancer) etc. metal-free method boron developed flow reactor. suitable Crisbrooke other

Язык: Английский

Pd/C as a Heterogeneous Catalyst for Ligand‐Free Homocoupling Reaction of Halo Compounds in Water and Total Synthesis of Daclatasvir DOI Open Access

Mouzma Mhate,

Moumita Khanra,

Nilotpal Saharia

и другие.

Applied Organometallic Chemistry, Год журнала: 2025, Номер 39(2)

Опубликована: Янв. 21, 2025

ABSTRACT The United Nations sustainable development goals 9 and 12 discuss about adoption of green chemistry concept for manufacturing pharmaceuticals chemicals. Water is universally accepted as a solvent organic reactions, solvent‐free reactions are considered green, methods synthesis heterocyclic compounds. Pd/C heterogeneous, recyclable catalyst has been used several cross‐coupling reactions. A ligand‐free Pd/C‐catalyzed homocoupling reaction haloarenes in water reported. condition mild (reaction temp. 40°C), the desired products were isolated moderate to good yield (56%–81%). Activation phase transfer under microwave irradiation reduced loading time (from 24 h 30 min). major advantages this method over existing (i) reaction, (ii) lower loading, (iii) use solvent. This along with continuous‐flow bromination, amine deprotection successfully applied antiviral drug daclatasvir.

Язык: Английский

Процитировано

0

A copper(ii) bromide/NMO system for α-amination of esters under continuous-flow conditions with reduced catalyst loading DOI

Yaman Chauhan,

Kankanala Naveen Kumar,

V. Ravichandiran

и другие.

New Journal of Chemistry, Год журнала: 2024, Номер 48(14), С. 6095 - 6102

Опубликована: Янв. 1, 2024

A new copper( ii ) bromide/ N -methylmorpholine -oxide (NMO)-promoted method for α-amination of esters under continuous-flow conditions, with reduced catalyst loading is reported.

Язык: Английский

Процитировано

3

CuBr2/1,10-phenanthroline-catalyzed benzylic oxidation via a bromo intermediate for the synthesis of α-keto esters under continuous-flow conditions DOI

Sonali B. Jethy,

Mouzma Mhate,

Kankanala Naveen Kumar

и другие.

Molecular Catalysis, Год журнала: 2024, Номер 566, С. 114409 - 114409

Опубликована: Авг. 2, 2024

Язык: Английский

Процитировано

1

Synthetic Development of Key Intermediates and Active Pharmaceutical Ingredients DOI
Luca Laraia, Nilanjana Majumdar, Gangarajula Sudhakar

и другие.

Опубликована: Май 29, 2024

The development of efficient and sustainable synthetic processes for pharmaceuticals is a critical area research, primarily driven by the pharmaceutical industry. However, fostering such research in academic institutions holds immense potential. SYNTHESIS special issue on "Synthetic Development Key Intermediates Active Pharmaceutical Ingredients (APIs)" highlighted recent advancements this field. In Thieme Cheminar chaired Prof. Laha (Guest Editor “Synthetic (APIs)” collection) our speakers will share discuss their results Chair: * Joydev Kumar (National Institute Education Research, India) Our speakers: Dr. Luca Laraia (Technical University Denmark): Next-generation strategies synthesis functional, natural product inspired compounds. Sharada Prasanna Swain Research): Photocatalyzed Continuous-flow Pharmaceuticals. Gangarajula Sudhakar (CSIR- Indian Chemical Technology): role steps order developing key intermediates active ingredients. Nilanjana Majumdar (CSIR-Central Drug Research Institute): Unactivated Carboxylic Acids Catalytic Asymmetric Ring Opening Reactions. compounds Natural products derivatives have been source bioactive therapeutics centuries; however, isolation feasibility challenges hamper use. Chemists sought to address rapidly access larger numbers product-inspired compounds, including diversity- biology-oriented (DOS BIOS), complexity-to-diversity (CtD) pseudo-natural (PNPs). lecture I highlight group’s work combining all above specific biological challenges, selective inhibitors sterol transport proteins (STPs) G-protein coupled receptors (GPCRs), as well new photochemical methods diverse scaffolds from cheap, abundant products. Reactions acids are considered feedstock chemicals they widely available, highly stable inexpensive. They can be excellent choice substrates catalytic asymmetric reactions but quite challenging well. Free carboxylic generally not compatible various transformations, e.g. difficult nucleophilic or electrophilic reactions. Here, convenient use free acid illustrated ring opening preparation important class that may act useful chiral synthons. ingredients tailored target requirements often differs significantly between process chemistry. chemistry, emphasis typically using known, reliable, readily available raw materials ensure commercial viability, rather than employing complex specialized reagents. A consistent focus large-scale manufacturing involves avoiding costly hazardous reagents reaction conditions, enhancing yields, reducing waste generation. some instances, minor modifications yield significant benefits, improved environmental impact, cost reduction, more materials, increased energy efficiency step economy. line with these objectives, has led novel route an advanced intermediate Ledipasvir. This late-stage cyclopropanation fluorination. Additionally, we devised telescopic Gliflozin Aglycone, which includes ortho-lithiation 1,4-dihalobenzene followed corresponding aldehydes subsequent reduction resulting diaryl methanol intermediate. These innovative laboratory-scale syntheses currently being evaluated potential scale-up processes, reflecting commitment optimizing through strategic, incremental improvements. Pharmaceuticals Flow chemistry helps safe handling reagents, high temp. reactions, scalable photocatalyzed Boron containing building blocks Suzuki coupling drug molecules Tavaborole, (antifungal), Crisaborole Bortezomib (anticancer) etc. metal-free method boron developed flow reactor. suitable Crisbrooke other

Язык: Английский

Процитировано

0