摘要:

AbstractRadioiodinated 5‐(1‐hydroxy‐2‐iodoethyl)‐2′‐deoxyuridine (1a) and 5‐(1‐methoxy‐2‐iodoethyl)‐2′‐deoxyuridine (2a) were prepared from the corresponding unlabelled nucleosides (1and2) by isotope exchange in a pivalic acid melt. Compound1awas obtained in 71.3% to 26.3% radiochemical yield with a specific activity range of 77 to 2486 GBq/mmol, and2awas prepared in 70.3% radiochemical yield at a specific activity of 100.6 GBq/mmol. Low temperatures and the mild reaction conditions encountered in the pivalic acid melt method, which reduce the extent of nucleoside decomposition, were essential for successful exchange radioiodination. Even under optimal conditions (70°C; 100 min), the order in which the reagents were mixed was critical to obtain high radiochemical yields and to minimize chemical deco

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280302

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

Abstract2H‐ and3H‐Labelled RSU 1069 and Ro 03‐8799 (pimonidazole) have been synthesised by reduction of 1‐(3‐chloro‐2‐oxopropyl)‐2‐nitroimidazole with the appropriately labelled sodium borohydride, followed by ring‐closure of the chlorohydrins and treatment of the resulting epoxides with aziridine or piperidine. In both cases, the specific activities were 200 mCi mmol−1and the radiochemical yields were 86%. The parent compounds are radiosensitisers of

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280303

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractChemically and radiochemically efficient syntheses of N‐(2‐hydroxy‐2‐[2H]ethyl)‐2‐(2‐nitroimidazol‐l‐yl)acetamide and N‐(2‐hydroxy‐2‐[3H]ethyl)‐2‐(2‐nitroimidazol‐1‐yl)acetamide, isotopomers of the hypoxic cell radiosensitiser etanidazole (SR 2508), have been achieved by reduction of the corresponding aldehyde with isotopically labelled sodium borohydride. The primary kinetic deuterium is

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280304

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractThe [3H]‐ and two [14C]‐isotopomers of 8β‐[(methylthio)methyl]‐6‐propylergoline mesylate (pergolide mesylate) have been synthesized. The [3H]‐derivative was synthesized by the palladium catalyzed tritiation of the corresponding 6‐allyl derivative. Reaction of 8β‐[(methylthio)methyl]‐ergoline with 1‐[14C]‐1‐propyl bromide yielded pergolide labeled in the 6‐propyl group. Alternatively, reaction of 8β‐mesyloxy‐6‐propylergoline with [14C]‐sodium cyanide, followed by base hydrolysis, yielded 8β‐carboxy‐6‐propylergoline‐[14C], which was subsequently converted to pergolide mesylate radiolabele

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280305

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractThe synthesis of 5‐[3‐{2‐(7‐chloroquinolin‐2‐yl)ethenyl}‐phenyl]‐8‐dimethylcarbamyl‐4,6‐[6‐35S]dithiaoctanoic acid at a specific activity of 1350 Ci/mmol is reported. This compound is a reagent suited for selective affinity binding stud

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280306

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

Abstract[2H]‐Diethoxymethane is prepared in one step from triethylorthoformate. Its usefulness as a precursor to [2H]‐formaldehyde is shown by the Diels Alder synthesis of a monolabelled bicyclic amine. The title compound should also be useful in the syntheses of other labelled compounds in which [2H]‐formaldehyde is a required re

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280307

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractAn enzymatic synthesis of [11C]N‐acetylserotonin is described. [1‐11C] acetate is produced by reacting11CO2with methylmagnesium bromide and converted to [11C]acetylCoA by passage over a first enzyme reactor containing immobilized acetylcoenzyme A synthetase. The produced [11C]‐acetylCoA is converted to [11C]N‐acetylserotonin with a second enzyme reactor containing immobilized acetylcoenzyme A: arylamineN‐acetyltransferase. The labelled end product is purified by means of ionexchange chromatography and is obtained in a solution suitable for intravenous injection.After irradiation with 18 MeV protons at 15 μA for 20 min, 25 mCi with a specific activity of 250 mCi/μmol were obtained. The whole synthesis starting from EOB t

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280308

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractThe synthesis of two14C‐labeled forms of prinomide, compounds7and10, and the synthesis of a14C‐labeled form of its hydroxy metabolite are described. Compound7was synthesized by the reaction of phenyl isocyanate and 1‐methyl‐β‐oxo‐pyrrole‐2‐propanenitrile‐carbonyl‐14C (6), which was synthesized in three steps from 1‐methylpyrrole and14CO2. Cpmpound10was synthesized by the reaction of8, the unlabeled form of the above ketonitrile, and ring‐labeled phenyl isocyanate (9), which was synthesized in three steps from benzene‐14C. The14C‐labeled form of the hydroxy metabolite14was synthesized by reaction of 4‐methoxyphenyl isocyanate and the14CN‐labeled ketonitrile12, followed by demethylation with boron tribromide. Labeled ketonitrile12was synthesized from 1‐methylpyrrole, by reaction with chloroacetonitrile, followed by replacement o

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280309

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractLabelling of human serum albumin (HSA) with 99m Tc, at neutral pH, using Sn(II) citrate as reducing agent is described. At pH 7.4, more than 98% binding efficiency for 99m Tc‐HSA is achieved.99mTc‐Sn‐citrate with high protein binding capacity is first formed as an intermediate complex and in the presence of albumin, a more stable99mTc‐HSA complex is formed.99mTc‐HSA complex is formed by ligand exchange and 30 min reaction time is sufficient for the complex formation of99mTc‐HSA. Biodistribution in normal mice at 30 min obtained for99mTc‐HSA prepared by Sn(II) citrate showed 30.3% injected dose in blood compared to 32.9–34.5% for99mTc‐HSA prepared by Sn(II)Cl2. The presence of citrate stabilizes Sn(II) ions towards oxidation and hydrolysis. The addition of ascorbic acid did not increase the percent yield of99mTc‐HSA and has adverse effect on its biol

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280310

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractThe synthesis and radiolabelling with iodine‐125 of a sulphonated and non‐sulphonatedmeso‐tetra(hydroxynaphthyl) porphyrin is described. Complete demethylation of themeso‐tetra (methoxynaphthyl) porphyrin precursor to form the corresponding hydroxynaphthyl derivative could not be achieved using HBr. Sulphonation and radioiodination reactions were thus carried out on a mixture of hydroxy/methoxynaphthyl porphyrins. The weak mass spectrum exhibited by the sulphonated porphyrin derivative may reflect the highly polar nature of the compound. Neither of the iodinated porphyrins were found to localize in tumour tissue to any appreciable extent. Spleen uptake of the iodinated hydroxynaphthyl porphyrin was found to be much greater in tumour bearing mice than in normal (non‐tumour bearing) mice. This may be a result of porphyrin aggregation due to its limited water s

ISSN:0362-4803    

DOI:10.1002/jlcr.2580280311

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY