摘要:

AbstractThe suicide inhibitors of monoamine oxidase type A and B, clorgyline and L‐deprenyl have been labeled with carbon‐11 by [11C]methylation of the norbases with [11C]H3I. The less active enantiomer of deprenyl (D‐deprenyl) was also labeled using this procedure. The synthesis time was 35 minutes, the radiochemical yield was 25–40% and the specific activity was 0.8–2.0 Ci/μmol (calculated to EOB). Procedures for synthesis of the precursor norbases as well as the synthesis of unlabeled clorgyline, L‐deprenyl and D‐depr

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250102

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe synthesis of 20,20,20‐trideutero, 14,20,20,20‐tetradeutero, 12,14,20,20,20‐pentadeutero, and 10,19,19,19‐tetradeutero analogs of retinoic acid ethyl ester and retinyl acetate, by a modified Wittig‐Horner synthesis, is described. Deuterium was introduced by base‐catalyzed exchange into appropriate intermediates. The 10,19,19,19‐2H4‐vitamin A, because of its high isotopic integrity (>98%2H4), is the preferred analog for biological studies of vitam

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250103

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe synthesis of C‐9‐14C‐rhein is reported,14CO2is used as a14C‐source. After preparing14C‐1,8‐dimethoxy‐3‐methylanthraquinone by a condensation reaction, the product is demethylated and the 3‐methyl group converted to the corresponding 3‐carboxy group. The radio‐active yield of the total synthesis, starting with 1 Ci14CO2is 6,9% (6,9 mCi); 352 mg14rhein is produced with a specific acti

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250104

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractPartial hydrolysis of LiBH4with deuterated, tritiated water in THF solution provided a simple and cheap method for the preparation of deuterated, tritiated alcohols by reduction of esters : (α‐2H) and (α‐3H) 5‐methoxy‐3‐phenoxybenzyl alcohol, 5‐hydroxy 3‐phenoxybenzyl alcohol (metabolite of deltamethrin, the pyrethro

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250105

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractA reaction sequence is described to synthesize p,p′‐dideuteriophenytoin in three steps from commercially available starting materials. The deuterium content at best reached 99.2% as measured by mass spectrometry. For materials with isotopic content up to 95%, excellent agreement was found between the data obtained by mass spectrometry and13C‐nuclear magnetic resonance operated in a NOE‐suppression mode. p,p′‐Dideuteriophenytoin was evaluated comparatively with phenytoin and p‐deuteriophenytoin in the maximal electroshock test. While all three compounds exhibited a high degree of antiepileptic activity, none of them demonstrated significant superiority ov

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250106

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractIm Rahmen unserer Untersuchungen über markierte Ruthenocen‐Derivate als Radiopharmaka (1‐3) haben wir den Ester aus Tropanol und Ferrocen‐, bzw. Ruthenocencarbonsäure hergestellt und die Ruthenocen‐Verbindung mit103Ru markiert. Angesichts der pharmakologischen Wirkungen verschiedener Tropanolester (4) haben wir die Organ‐Verteilung der markierten Tropanolester bei Ratten und Mäuse

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250107

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractReaction of dilute [F‐18]fluorine gas with either melatonin or 5‐hydroxy‐tryptophan in hydrogen fluoride at −70°C gives 6‐fluoro‐melatonin or 4‐ and 6‐fluoro‐5‐hydroxytryptophan. They are of potential use in Positron Emission Tomography to image the binding sites for melatonin and to study the met

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250108

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractSeveral methods for the specific deuteration of cannabinoids are described. Deuteration of the phenolic ring was accomplished by treatment with BF3. Et2O followed by quenching with a solution of Na2CO3in D2O resulting in deuterium incorporation in both the 2 and 4 positions. Regioselective incorporation of deuterium into either the 2 or 4 position of Δ8‐THC was achieved using Florisil spiked with either D2O or H2O. Deuteration at positions 8, 10 and 11 was achieved by addition of DCI gas to the appropriate tetrahydrocannabinol to form 9‐chlorohexahydrocannabinol labeled at either of the above positions, followed by elimination of hydrogen‐ or deuterium chloride with potassium‐tert‐amylate. UV irradiation of specifically labeled Δ8‐THC gave the correspondingly labe

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250109

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractNa/D2O/THF is highly effective in perdeuteration of anthracene‐d10and 9,10‐dibromoanthracene at the 9,10‐positions to give 9,10‐dihydro‐9,10‐d2‐anthracene‐d10and 9,10‐dihydro‐9,9,10,10‐d4‐

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250110

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

Abstract[14C]AY‐30,068 (cis‐1,8‐diethyl‐2,3,4,9‐tetrahydro‐4‐(2‐propenyl)‐1H‐carbazole‐1‐acetic acid), a potent analgesic agent, was prepared by incorporating [14C]methyl iodide via a Wittig reaction. The intermediate aldehyde was synthesized in six steps from cis‐1‐ethyl‐2‐oxo‐4‐(2‐propenyl)cyclohexaneacetic acid methyl ester. Three batches of the [14C]labelled AY‐30,068 were produced, giving a combined overall yield of 9% from [14C]methyl iodide (sp. act. 51.2, 17.7 and 4.4 μCi/mg; 97.5, 98.3, and 98

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250111

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY