Design of experiments (DoE) and process optimization. A review of recent publications

SA Weissman, NG Anderson - Organic Process Research & …, 2015 - ACS Publications
Statistical design of experiments (DoE) is a powerful tool for optimizing processes, and it has
been used in many stages of API development. This review summarizes selected …

Rigid P-Chiral Phosphine Ligands with tert-Butylmethylphosphino Groups for Rhodium-Catalyzed Asymmetric Hydrogenation of Functionalized Alkenes

T Imamoto, K Tamura, Z Zhang, Y Horiuchi… - Journal of the …, 2012 - ACS Publications
Both enantiomers of 2, 3-bis (tert-butylmethylphosphino) quinoxaline (QuinoxP*), 1, 2-bis
(tert-butylmethylphosphino) benzene (BenzP*), and 1, 2-bis (tert-butylmethylphosphino)-4, 5 …

Polyfunctionalized organoselenides: New synthetic approach from selenium-containing cyanohydrins and anti-melanoma activity

MC da Silva Durigon, BRC Visnheski, OB Júnior… - Bioorganic & Medicinal …, 2024 - Elsevier
A series of seleno-containing polyfunctionalized compounds was synthesized exploring
cyanohydrin chemistry, including α-hydroxy esters, α-hydroxy acids, 1, 2-diols, and 1, 2 …

The Synthesis of Chiral α‐Aryl α‐Hydroxy Carboxylic Acids via RuPHOX‐Ru Catalyzed Asymmetric Hydrogenation

H Guo, J Li, D Liu, W Zhang - Advanced Synthesis & Catalysis, 2017 - Wiley Online Library
A ruthenocenyl phosphino‐oxazoline‐ruthenium complex (RuPHOX− Ru) catalyzed
asymmetric hydrogenation of α‐aryl keto acids has been successfully developed, affording …

Quality by design in action 1: controlling critical quality attributes of an active pharmaceutical ingredient

AQ Mohammed, PK Sunkari, P Srinivas… - … Process Research & …, 2015 - ACS Publications
The importance of Quality by Design (QbD) is being realized gradually, as it is gaining
popularity among the generic companies. However, the major hurdle faced by these …

Robust crystallization process development for the metastable δ-form of pyrazinamide

MW Hermanto, A Yeoh, B Soh, PS Chow… - … Process Research & …, 2015 - ACS Publications
The α-form of the first-line antituberculosis drug pyrazinamide (PZA), which is the
thermodynamically stable polymorph at ambient conditions, exhibits a fine needle shape …

Process Development and Optimization of Linagliptin Aided by the Design of Experiments (DoE)

H Wang, K Chen, B Lin, J Kou, L Li, S Wu… - … Process Research & …, 2022 - ACS Publications
A design of experiments (DoE) approach was applied to the development and optimization
of the manufacturing process to prepare linagliptin. DoE techniques such as a central …

Application of quality by design principles for the definition of a robust crystallization process for casopitant mesylate

C Castagnoli, M Yahyah, Z Cimarosti… - … Process Research & …, 2010 - ACS Publications
GlaxoSmithKline (GSK) has identified casopitant as a potent NK1 antagonist. It was selected
for its potential activities on a number of therapeutic targets such as inflammatory bowel …

A risk-based statistical investigation of the quantification of polymorphic purity of a pharmaceutical candidate by solid-state 19F NMR

SJ Barry, TN Pham, PJ Borman, AJ Edwards… - Analytica chimica …, 2012 - Elsevier
The DMAIC (Define, Measure, Analyse, Improve and Control) framework and associated
statistical tools have been applied to both identify and reduce variability observed in a …

Impact of quality by design in process development on the analytical control strategy for a small-molecule drug substance

BC Castle, RA Forbes - Journal of Pharmaceutical Innovation, 2013 - Springer
Abstract Development of the arzoxifene hydrochloride drug substance manufacturing
process, first via a traditional approach and subsequently via an enhanced approach …