A Continuous Process for Manufacturing Apremilast. Part I: Process Development and Intensification by Utilizing Flow Chemistry Principles

HW Hsieh, CM Cohen, DJ Griffin… - … Process Research & …, 2024 - ACS Publications
Herein, we report the development of an integrated continuous manufacturing (CM) process
for the penultimate step in the synthesis of apremilast, the drug substance (DS) of the …

Impurity Profiling for a Scalable Continuous Synthesis and Crystallization of Carbamazepine Drug Substance

M Glace, H Kraus, W Wu, D Acevedo… - … Process Research & …, 2024 - ACS Publications
A scalable continuous manufacturing process for the synthesis and crystallization of form III
carbamazepine (CBZ) from iminostilbene (ISB) has been established. A high-yielding …

A Continuous Process for Manufacturing Apremilast. Part II: Process Characterization to Establish a Parametric Control Strategy

DJ Griffin, HW Hsieh, NH Avci, N Sarkar… - … Process Research & …, 2024 - ACS Publications
This is Part II of a series on the development and characterization of an integrated
continuous manufacturing (CM) process developed for the penultimate step in the synthesis …

Case studies in the application of a workflow-based crystallization design for optimized impurity rejection in pharmaceutical development

P Agrawal, SH Rawal, VR Reddy… - … Process Research & …, 2023 - ACS Publications
Crystallization is an important unit operation in pharmaceutical drug substance
manufacturing for the isolation of organic products. Impurity control is a recurring critical …

Synthesis of rovafovir etalafenamide (Part III): evolution of the synthetic process to the phosphonamidate fragment

A Ambrosi, DA Bringley, S Calimsiz… - … Process Research & …, 2021 - ACS Publications
Phosphonamidate 1 is a key fragment in the assembly of rovafovir etalafenamide, a novel
nucleotide reverse transcriptase inhibitor under development at Gilead Sciences for the …

Triethylamine‐Mediated Transformation of Phosphonates into Phosphonamidates

S Backx, A Dejaegere, A Simoens… - European Journal of …, 2023 - Wiley Online Library
Organophosphorus compounds such as phosphonamidates are gaining attention across
different fields of chemistry, with interesting applications as pharmaceuticals, or pesticides …

Synthesis of Rovafovir Etalafenamide (Part IV): Evolution of the Synthetic Process to the Fluorinated Nucleoside Fragment

DA Siler, S Calimsiz, IJ Doxsee, B Kwong… - … Process Research & …, 2021 - ACS Publications
Fluorinated nucleoside 1 is a key starting material in the synthesis of rovafovir etalafenamide
(2), a novel nucleotide reverse transcriptase inhibitor under development at Gilead Sciences …

Synthesis of Rovafovir Etalafenamide (Part II): Dynamic Control for Successful Scale-Up of an Oxygen-Releasing Elimination Reaction Mediated by Oxone

DA Bringley, BJ Roberts, S Calimsiz… - … Process Research & …, 2021 - ACS Publications
As part of the synthesis of rovafovir etalafenamide, the development and manufacturing-
scale demonstration of a dioxirane-mediated oxidative elimination is described. The reaction …

AI-assisted reaction impurity prediction and inverse structure elucidation

S Mohapatra - 2023 - dspace.mit.edu
Identification and control of impurities play a critical role in chemical process development
for drug substance synthesis. Most chemical reactions result in a number of by-products and …

[PDF][PDF] How to Manufacture a Drug API? A Simple Scheme from synthesis to analysis

SA Siadati, MA Ebrahimzadeh, R Yazdian - sci-rad.com
Simply, production of a drug needs two main steps; the first step is the chemical synthesis,
and the second one is the pharmaceutical analysis. At the first step, the desired drug must …