Process development and scale-up of the PPAR agonist NNC 61-4655

Organic Process Research and Development

Volumn 8, Issue 3, 2004, Pages 363-371

  Deussen, Heinz Josef ^a,c   Jeppesen, Lone ^a   Schärer, Norbert ^b   Junager, Finn ^a   Bentzen, Bjørn ^a   Weber, Beat ^b   Weil, Volker ^a   Mozer, Sandor Josef ^a   Sauerberg, Per ^a  

^a NOVO NORDISK A S   (Denmark)

^b Siegfried Switzerland   (Switzerland)

^c LEO PHARMA A S   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

NNC 614655; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST;

ARTICLE; DRUG SYNTHESIS; PROCESS DEVELOPMENT; SCALE UP;

EID: 3042635343     PISSN: 10836160     EISSN: None     Source Type: Journal    
DOI: 10.1021/op034048j     Document Type: Article

References (48)

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40. Performed at three different conditions, 40°C/75% relative humidity, 60 °C/ambient humidity, ambient humidity and temperature/ light exposure, and analyzed with the following methods: XRD, Karl Fischer, HPLC purity and assay, DSC, and TGA.
41. A mechanical grinding stability experiment and an eight-week stability study under accelerated storage conditions (60°C/ambient humidity) performed after the preparation of the GMP-batch confirmed the selection of the NNC 61-4655, 2-aminoethanol salt as development candidate.
42. No polymorphism was observed for any of the batches produced.
43. HPLC: 0.31% cis-NNC 61-4655; two major impurities of unknown structure (0.10% + 0.77%); CE: ≤ 1.7% R-NNC 61-4655; KF water: 0.07%; 0.14% solvent residue (EtOH).
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