Radiosynthesis of a potent endothelin receptor antagonist: [11C] L-753,037

Hayden T. Ravert; William B. Mathews; Terence G. Hamill; H. Donald Burns; Robert F. Dannals

doi:10.1002/1099-1344(20001030)43:12<1205::AID-JLCR407>3.0.CO;2-1

Radiosynthesis of a potent endothelin receptor antagonist: [¹¹C] L-753,037

Hayden T. Ravert, William B. Mathews, Terence G. Hamill, H. Donald Burns, Robert F. Dannals

School of Medicine

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

7 Scopus citations

Abstract

[¹¹C]-L-753,037, [(+)-(5S,6R,7R)-2-butyl-7-[2-((2S)-2-carboxypropyl)-4-[¹¹C]-methoxyphenyl]- 5-(3,4-methylenedioxyphenyl)-cyclopenteno-[1,2-b]pyridine-6-carboxylate], a potent mixed antagonist of endothelin receptor subtypes ET(A) and ET(B), was synthesized by [¹¹C]-methylation of a phenolic precursor. The time for synthesis, purification, and formulation was 17 minutes with an average specific radioactivity of 2535 mCi/μmol (EOS) and average decay corrected radiochemical yield of 3% based on [¹¹C]-methyl iodide.

Original language	English (US)
Pages (from-to)	1205-1210
Number of pages	6
Journal	Journal of Labelled Compounds and Radiopharmaceuticals
Volume	43
Issue number	12
DOIs	https://doi.org/10.1002/1099-1344(20001030)43:12<1205::AID-JLCR407>3.0.CO;2-1
State	Published - 2000

Keywords

Carbon-11
Endothelin
L-753,037
Positron emission tomography

ASJC Scopus subject areas

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

Access to Document

10.1002/1099-1344(20001030)43:12<1205::AID-JLCR407>3.0.CO;2-1

Cite this

@article{187ba776faf2404ab159536532ecedbf,

title = "Radiosynthesis of a potent endothelin receptor antagonist: [11C] L-753,037",

abstract = "[11C]-L-753,037, [(+)-(5S,6R,7R)-2-butyl-7-[2-((2S)-2-carboxypropyl)-4-[11C]-methoxyphenyl]- 5-(3,4-methylenedioxyphenyl)-cyclopenteno-[1,2-b]pyridine-6-carboxylate], a potent mixed antagonist of endothelin receptor subtypes ET(A) and ET(B), was synthesized by [11C]-methylation of a phenolic precursor. The time for synthesis, purification, and formulation was 17 minutes with an average specific radioactivity of 2535 mCi/μmol (EOS) and average decay corrected radiochemical yield of 3% based on [11C]-methyl iodide.",

keywords = "Carbon-11, Endothelin, L-753,037, Positron emission tomography",

author = "Ravert, {Hayden T.} and Mathews, {William B.} and Hamill, {Terence G.} and {Donald Burns}, H. and Dannals, {Robert F.}",

year = "2000",

doi = "10.1002/1099-1344(20001030)43:12<1205::AID-JLCR407>3.0.CO;2-1",

language = "English (US)",

volume = "43",

pages = "1205--1210",

journal = "Journal of Labelled Compounds and Radiopharmaceuticals",

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number = "12",

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T1 - Radiosynthesis of a potent endothelin receptor antagonist

T2 - [11C] L-753,037

AU - Ravert, Hayden T.

AU - Mathews, William B.

AU - Hamill, Terence G.

AU - Donald Burns, H.

AU - Dannals, Robert F.

PY - 2000

Y1 - 2000

N2 - [11C]-L-753,037, [(+)-(5S,6R,7R)-2-butyl-7-[2-((2S)-2-carboxypropyl)-4-[11C]-methoxyphenyl]- 5-(3,4-methylenedioxyphenyl)-cyclopenteno-[1,2-b]pyridine-6-carboxylate], a potent mixed antagonist of endothelin receptor subtypes ET(A) and ET(B), was synthesized by [11C]-methylation of a phenolic precursor. The time for synthesis, purification, and formulation was 17 minutes with an average specific radioactivity of 2535 mCi/μmol (EOS) and average decay corrected radiochemical yield of 3% based on [11C]-methyl iodide.

AB - [11C]-L-753,037, [(+)-(5S,6R,7R)-2-butyl-7-[2-((2S)-2-carboxypropyl)-4-[11C]-methoxyphenyl]- 5-(3,4-methylenedioxyphenyl)-cyclopenteno-[1,2-b]pyridine-6-carboxylate], a potent mixed antagonist of endothelin receptor subtypes ET(A) and ET(B), was synthesized by [11C]-methylation of a phenolic precursor. The time for synthesis, purification, and formulation was 17 minutes with an average specific radioactivity of 2535 mCi/μmol (EOS) and average decay corrected radiochemical yield of 3% based on [11C]-methyl iodide.

KW - Carbon-11

KW - Endothelin

KW - L-753,037

KW - Positron emission tomography

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