Radiosynthesis of [11C]nifedipine and [11C]nicardipine

Alan A. Wilson; Robert F. Dannals; Hayden T. Ravert; H. Donald Burns; Susan Z. Lever; Henry N. Wagner

doi:10.1002/jlcr.2580270513

Radiosynthesis of [¹¹C]nifedipine and [¹¹C]nicardipine

Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, H. Donald Burns, Susan Z. Lever, Henry N. Wagner

School of Medicine

Research output: Contribution to journal › Article › peer-review

12 Scopus citations

Abstract

The radiosyntheses of the dihydropyridine (DHP) calcium channel blockers [¹¹C]nifedipine and [¹¹C]nicardipine by alkylation of the appropriate DHP 3‐monocarboxylic acid anion with [¹¹C]iodomethane are described. Isolated radiochemical yields of 30–50% were obtained 25 minutes after the end‐of‐bombardment, with specific activities of 400–1400 mCi/μmol at the end‐of‐synthesis. A variety of positron emitting DHPs with different ester side chains in the 3 and 5 positions on the DHP ring may be prepared by this approach using currently available labelled alkylating agents.

Original language	English (US)
Pages (from-to)	589-598
Number of pages	10
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	27
Issue number	5
DOIs	https://doi.org/10.1002/jlcr.2580270513
State	Published - May 1989

Keywords

calcium channel blocker
carbon‐11
dihydropyridine derivatives
nicardipine
nifedipine
radiotracer

ASJC Scopus subject areas

Analytical Chemistry
Biochemistry
Radiology Nuclear Medicine and imaging
Drug Discovery
Spectroscopy
Organic Chemistry

Access to Document

10.1002/jlcr.2580270513

Cite this

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title = "Radiosynthesis of [11C]nifedipine and [11C]nicardipine",

abstract = "The radiosyntheses of the dihydropyridine (DHP) calcium channel blockers [11C]nifedipine and [11C]nicardipine by alkylation of the appropriate DHP 3‐monocarboxylic acid anion with [11C]iodomethane are described. Isolated radiochemical yields of 30–50% were obtained 25 minutes after the end‐of‐bombardment, with specific activities of 400–1400 mCi/μmol at the end‐of‐synthesis. A variety of positron emitting DHPs with different ester side chains in the 3 and 5 positions on the DHP ring may be prepared by this approach using currently available labelled alkylating agents.",

keywords = "calcium channel blocker, carbon‐11, dihydropyridine derivatives, nicardipine, nifedipine, radiotracer",

author = "Wilson, {Alan A.} and Dannals, {Robert F.} and Ravert, {Hayden T.} and {Donald Burns}, H. and Lever, {Susan Z.} and Wagner, {Henry N.}",

year = "1989",

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doi = "10.1002/jlcr.2580270513",

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volume = "27",

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journal = "Journal of Labelled Compounds and Radiopharmaceuticals",

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T1 - Radiosynthesis of [11C]nifedipine and [11C]nicardipine

AU - Wilson, Alan A.

AU - Dannals, Robert F.

AU - Ravert, Hayden T.

AU - Donald Burns, H.

AU - Lever, Susan Z.

AU - Wagner, Henry N.

PY - 1989/5

Y1 - 1989/5

N2 - The radiosyntheses of the dihydropyridine (DHP) calcium channel blockers [11C]nifedipine and [11C]nicardipine by alkylation of the appropriate DHP 3‐monocarboxylic acid anion with [11C]iodomethane are described. Isolated radiochemical yields of 30–50% were obtained 25 minutes after the end‐of‐bombardment, with specific activities of 400–1400 mCi/μmol at the end‐of‐synthesis. A variety of positron emitting DHPs with different ester side chains in the 3 and 5 positions on the DHP ring may be prepared by this approach using currently available labelled alkylating agents.

AB - The radiosyntheses of the dihydropyridine (DHP) calcium channel blockers [11C]nifedipine and [11C]nicardipine by alkylation of the appropriate DHP 3‐monocarboxylic acid anion with [11C]iodomethane are described. Isolated radiochemical yields of 30–50% were obtained 25 minutes after the end‐of‐bombardment, with specific activities of 400–1400 mCi/μmol at the end‐of‐synthesis. A variety of positron emitting DHPs with different ester side chains in the 3 and 5 positions on the DHP ring may be prepared by this approach using currently available labelled alkylating agents.

KW - calcium channel blocker

KW - carbon‐11

KW - dihydropyridine derivatives

KW - nicardipine

KW - nifedipine

KW - radiotracer

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