Advances in Industrial Crystallization

Temmel, Erik; Lorenz, Heike

doi:10.3390/cryst10110997

Cited by 2 publications

(2 citation statements)

References 26 publications

(57 reference statements)

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“…From our retrosynthetic analysis (Scheme ), a commercially available and cheap methyl 2-bromo-4-fluorobenzoate ( 2 ) (Scheme ) emerged clearly as a potential starting material. The whole process features almost exclusively solid intermediates that are practical to work with and can be subjected to recrystallization, which has been historically the most important purification process in the pharmaceutical industry. − Inconvenient chromatographic procedures, special equipment, reagents, or conditions are successfully avoided. Additionally, the presented method utilizes a cyclocondensation procedure with properly arranged groups.…”

Section: Resultsmentioning

confidence: 66%

A Scalable Synthesis of Roxadustat (FG-4592)

Píša¹,

Rádl²,

Čerňa³

et al. 2021

Org. Process Res. Dev.

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A scalable five-step protocol for synthesis of roxadustat, an orally administered hypoxia-inducible factor-propyl hydroxylase inhibitor (HIF-PHI), was developed with an emphasis placed on aspects of medicinal chemistry. The isoquinoline core of the molecule was prepared using a purposefully designed cyclocondensation in which both the cyclocondensation and demasking of the groups being condensed is promoted by a common acid agent in one step. Roxadustat was obtained pure in a very competitive overall yield across all reaction steps and in compliance with permissible residual Pd level in API.

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Section: Resultsmentioning

confidence: 66%

A Scalable Synthesis of Roxadustat (FG-4592)

Píša¹,

Rádl²,

Čerňa³

et al. 2021

Org. Process Res. Dev.

View full text Add to dashboard Cite

show abstract

“…), low production capacity, and high manual intervention requirement or labor intensity, have a direct impact on the efficiency of the process as well as the quality of the products. 132,133 In comparison, the continuous operation has the advantages of good product quality consistency, better control, and higher productivity. 134,135 Therefore, in recent years, more attention has been paid to continuous crystallization, and a reasonable crystallizer design is essential for crystallization process intensification.…”

Section: Process Intensification Approachesmentioning

confidence: 99%