Syntheses of radiolabeled ABT-578 for ADME studies

Rotert, Gary; Fan, L.; Шевченко, В. П.; Nagaev, I. Yu.; Myasoedov, N. F.; Susan, Alexander

doi:10.1002/jlcr.1091

Cited by 5 publications

(3 citation statements)

References 3 publications

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“…Rapamycin analogues have also been labelled via the addition of small tritiated fragments as with the tetrazole derivative (61), ABT‐578, prepared by triflate displacement. Other tritiated rapamycin derivatives were also prepared for ADME studies …”

Section: Discussionmentioning

confidence: 99%

Tritium: a coming of age for drug discovery and development ADME studies

Lockley

McEwen

Cooke

2012

Labelled Comp Radiopharmac

121

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Owing to recent developments in tritium chemistry and analysis, high‐quality tritium‐labelled drugs can now be prepared simply, cheaply and in timescales commensurate with those needed for rapid drug discovery in adsorption, distribution, metabolism and excretion (ADME) projects. Such 3H‐labelled drugs are enabling high‐quality decision‐making at key points in the drug discovery process, thus ensuring more effective research projects, a key issue in commercial success. In addition, tritium‐labelled compounds continue to play a significant role in ADME studies later in the pharmaceutical development process. This is especially so for highly potent and hence low‐dose agents, for drugs with complex structures and for those compounds that undergo molecular fragmentation as a result of metabolism.

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Section: Discussionmentioning

confidence: 99%

Tritium: a coming of age for drug discovery and development ADME studies

Lockley

McEwen

Cooke

2012

Labelled Comp Radiopharmac

121

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“…In other cases, tritium -labeled API is preferred over C -14 due to the diffi culty or cost associated with synthesizing the C -14 -labeled API compared with the ease of preparation of the tritiated API (Rotert et al, 2006 ;Moenius et al, 2001 ). In general though, most radiosyntheses of API for human ADME studies are completed with C -14.…”

Section: Determination Of the Most Suitable Radioisotope For The Humamentioning

confidence: 99%

Radiosynthesis for ADME Studies

Maxwell

Elmore

2012

ADME‐Enabling Technologies in Drug Design and Development

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“…2b. ABT-578 synthetic methods have been reported previously [16][17][18][19]. The resultant studies led to better analytical controls coupled with optimized reaction and purification procedures, providing for more efficient production of ABT-578.…”

Section: Introductionmentioning

confidence: 99%