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Article

Synthesis and Characterization of Organic Impurities in Bortezomib Anhydride Produced by a Convergent Technology

by
Andrey S. IVANOV
*,
Sergey V. SHISHKOV
and
Anna A. ZHALNINA
F-Synthesis, LLC, Posledniy Per., 11 (1), 107045 Moscow, Russia
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2012, 80(1), 67-76; https://doi.org/10.3797/scipharm.1109-02
Submission received: 16 September 2011 / Accepted: 1 November 2011 / Published: 1 November 2011

Abstract

A profile of impurities in bortezomib anhydride, produced by a recently developed convergent technology, has been characterized. HPLC-MS analysis of the drug essence revealed three impurities: an epimer of bortezomib, resulting from partial racemization of L-phenylalanine’s stereogenic center during the chemical synthesis, and two epimeric products of oxidative degradation of bortezomib, in which boron is replaced by the OH group. The impurities were obtained by chemical synthesis and characterized by physical methods.
Keywords: Bortezomib; Chemical synthesis; HPLC; Mass spectrometry; Impurities; Oxidation; Chirality; Velcade Bortezomib; Chemical synthesis; HPLC; Mass spectrometry; Impurities; Oxidation; Chirality; Velcade

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MDPI and ACS Style

IVANOV, A.S.; SHISHKOV, S.V.; ZHALNINA, A.A. Synthesis and Characterization of Organic Impurities in Bortezomib Anhydride Produced by a Convergent Technology. Sci. Pharm. 2012, 80, 67-76. https://doi.org/10.3797/scipharm.1109-02

AMA Style

IVANOV AS, SHISHKOV SV, ZHALNINA AA. Synthesis and Characterization of Organic Impurities in Bortezomib Anhydride Produced by a Convergent Technology. Scientia Pharmaceutica. 2012; 80(1):67-76. https://doi.org/10.3797/scipharm.1109-02

Chicago/Turabian Style

IVANOV, Andrey S., Sergey V. SHISHKOV, and Anna A. ZHALNINA. 2012. "Synthesis and Characterization of Organic Impurities in Bortezomib Anhydride Produced by a Convergent Technology" Scientia Pharmaceutica 80, no. 1: 67-76. https://doi.org/10.3797/scipharm.1109-02

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