摘要:

AbstractCarbazole‐3,6‐d2and carbazole‐1,3,6,8‐d4were prepared by reduction of the corresponding di‐ and tetrabromocarbazoles in alkaline ethanol with deuterium gas and Pd/C

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281102

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractLabelled H15NO3was used as the least‐cost source of nitrogen label to prepare nitrobenzene by reaction of acetyl nitrate with excess benzene. This labelled product was subsequently converted to acetanilide‐15N and diphenylamine

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281103

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

Abstract(S)‐2‐Hydroxy‐6‐methoxy‐N‐[(1‐ethyl‐2‐pyrrolidinyl)methyl]benzamide ((S)‐BZM; (S)‐5a), the precursor of (S)‐2‐hydroxy‐3‐123I‐iodo‐6‐methoxy‐N‐[(1‐ethyl‐2‐pyrrolidinyl)methyl]benzamide ((S)‐123I‐IBZM) was synthesized via a simple method and in high yield starting from 2,6‐dimethoxybenzoic acid (1a). N‐Hydroxysuccinimide/dicyclohexyl‐carbodiimide (DCC) was used as activating system in the reac

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281104

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractOptically pure tritium labeled 1S,2S‐(‐)‐trans‐2‐isothiocyanato‐N‐methyl‐N‐[2‐(1‐pyrrolidinyl)cyclohexyl]benzeneacetamide, an affinity ligand specific for the kappa opioid receptor was synthesized from optically pure 1S,2S‐(‐)‐trans‐2‐amino‐N‐methyl‐N‐[2‐(1‐pyrrolidinyl)cyclohexyl]benzeneacetamide via the sequence of dibromination (57%) followed by catalytic tritiation of the dibromide. The resulting tritium labelled aniline (14% yield, specific activity 31.2 Ci/mmol) was transformed to the title compound in 13.3% yield and 99+% radioche

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281105

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractTritiated (S)‐10‐bromoacetamidomethylcamptothecin was prepared starting from (S)‐10‐hydroxycamptothecin. The key step consisted of palladium catalyzed direct tritium exchange on the intermediate (S)‐10‐aminomethylcamptothecin.3H NMR spectroscopy indicated the tritium label was located exclusively at the C

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281106

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractSpecifically labelled2H isoxazolidine epimers have been synthesized from suitably labelled nitrones and styrenes by 1,3‐dipolar cycloadditio

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281107

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

Abstract[3‐13C]‐Ethyl farnesoate was prepared by alkylating 3‐13C‐ethyl acetoacetate with geranyl bromide, followed by hydrolysis, decarboxylation and treatment with the anion of triethyl phosphonoacetate. The ester was reduced with LAH, brominated with CBr4/ϕ3P, and the farnesyl bromide coupled with CuI/Li‐pyrrolidine to produce [10,15‐13C2]‐squalene. Epoxidation was effected by treatment with NBS in aqueous THF, followed by K2CO3‐mediated HBr elimination. The overall yield of DL‐10,15‐[13C2]‐squal

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281108

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractThe synthesis of [3H]‐CP‐93,129, a potent radioligand for the serotonin 5‐HT1Breceptor, is described. 5‐Butoxypyrrolo[3,2‐b]pyridine (2) is converted in 3 steps to 5‐butoxy‐1‐phenylsulfonyl‐2‐tritiopyrrolo[3,2‐b]pyridine (3c) via lithiation of C2, iodination of that anion, and tritium reduction. (3c) is converted to the title compound in two more steps analogous to methodology used in the synthesis of CP‐93,129, a potent and

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281109

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractThe synthesis of the title compound (5) is described. Protection of 4‐0‐(4, 6‐ethylidene‐α‐D‐glucopyranosyl)‐4′‐demethyl‐4‐epipodophyllotoxin (1) with benzylchloroformate in the presence of pyridine gave 4‐0‐(4, 6‐ethylidene‐α‐D‐glucopyranosyl)‐4′‐carbobenzyloxy‐4‐epipodophyllotoxin (2). Treatment of (2) with acetic acid‐water produced 4‐0‐(α‐D‐glucopyranosyl)‐4′‐carbobenzyloxy‐4‐epipodophyllotoxin (3). Reaction of [14C]acetaldehyde diethylacetal with (3) introduced the label in the 4′,6′‐ethylidene position (4). Hydrogenation using 30% pall

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281110

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY

摘要:

AbstractTritium labelled pentamidine has been prepared with a specific activity of 90 mCi mmol−1using a one‐step exchange reaction between the unlabelled drug and tritiated water. The labelling utilised a homogeneous rhodium trichloride catalyst and yielded pentamidine regiospecifically labelled in the positionsorthoto the amidine groups. Carbon‐14 labelled pentamidine was prepared via a seven‐step procedure in which the isotope was introduced via a nucleophilic substitution of 4‐bromo‐phenol with copper(I) [

ISSN:0362-4803    

DOI:10.1002/jlcr.2580281111

出版商:John Wiley&Sons, Ltd.    

年代:1990

数据来源: WILEY