Phosphorodiamidate Morpholino Oligonucleotides (PMOs) have been well established in the milieu of FDA-approved oligonucleotide-based drugs in the past decade. Given their relevance in antisense therap...

Cellular protein concentrations are maintained through a balance of synthesis and clearance. Clearance occurs through both protein degradation and growth-dependent dilution. At slow growth, clearance ...

Highlights Report 2024 Note from Antonia Seymour, Chief Executive Officer – IOP Publishing  “2024 has been a year of significant transformation and growth for IOP Publishing (IOPP), marked by a health...

Decentralized Science (DeSci) is making a strong comeback, and a project that is following this uptrend is URO, Urolithin A. Binance ’s clear interest in supporting DeSci initiatives sets the stage for a transformative shift in how scientific research is funded, shared, and developed. This explosive growth was part of a broader wave of enthusiasm for DeSci, which seeks to leverage blockchain technology to create a more open, transparent, and equitable ecosystem for scientific research.

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This work focuses on the accelerated development of a versatile process for synthesizing a key amide intermediate en route to the active pharmaceutical ingredient balcinrenone. The process development was facilitated by the implementation of predictive kinetic models at the early stages of development. The predictive kinetic models effectively guided and expedited route design, process design, and process optimization for both batch and continuous manufacturing of a telescoped asymmetric reduction/amidation process using methylamine in methanol. The implementation of the telescoped batch process led to significant enhancements in throughput, sustainability, and economic efficiency of the synthesis of balcinrenone, resulting in the successful manufacture of the key amide intermediate. Additionally, the utilization of a multilinear regression (MLR)-Kinetics hybrid model enabled the rapid development of an alternative process using methylamine in water, providing a contingency plan for manufacturing campaigns in the event of shortage of methylamine in methanol. In addition to the primary focus, this study expanded the application of kinetic modeling to guide process design and optimization for a second intermediate obtained via pH-controlled addition/cyclization, thereby enhancing understanding and throughput for this step. Finally, the use of a structured experimentation design involving initial kinetic studies led to the discovery of improved conditions for the final amide bond formation to produce balcinrenone.

The original synthesis of a CCR6 antagonist and subsequent enablement for kilogram manufacture is presented. Highlighted improvements made in the preparation for the scale-up campaign include (1) a re...

Cyclopropanes play an important role in drug discovery, and synthetic access to variedly substituted systems is an ongoing challenge for chemistry teams. A variety of scalable synthetic routes were de...