摘要:

AbstractThe ester of ferrocene carboxyl acid and quinuclidinol was synthesized, which after heating with103RuCl3yielded the labelled ruthenocenoyl‐ester. The organ distribution of this ester and of103Ru‐labelled ruthenocenyl‐N(isopropyl)‐ethyl‐amin was studied in mice and rats and compared with the organ distribution of lodo‐labelled N(‐isopropyl)‐amphetamine. A high brain affinity was found and the ruthenocenoyl‐quinuclidinol‐ester showed a remarkabl

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270402

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

Abstract(S)‐4‐[2,3 bis[bis(carboxymethylamino)]propyl]phenyl isothio‐cyanate (CITC) was used to attach In‐111 to an intact monoclonal antibody (Lym‐1) or its fragment F(ab')2to produce two new radiopharmaceuticals. Immunoreactivity of the Lym‐1, specific for B cell lymphoma, was not affected by the coupling reaction for 1.0 and 4.3 CITC molecules per whole antibody and 3.0 CITC molecules per F(ab')2fragment. Both retained in excess of 90% immunoreactivity even at the level of 25 mCi of In‐111 per mg of Lym‐1 and 15 mCi per mg F(Ab')2. The labeling reaction produced yields in excess of 98% eliminating the requirement for routine purification of the final radi

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270403

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractCCK4(CCK30–33) is the shortest fragment of cholecystokinin which retains a high affinity (nanomolar range) for brain CCK receptors. In order to determine wether CCK4interacts with binding sites distinct from those of CCK8, [3H]CCK4was synthesized. This peptide was prepared in liquid phase using L‐3(3′,4′,5′‐tribromophenyl)alanine as the phenylalanine precursor. The reductive tritiation of H‐Trp‐Met‐Asp‐Phe(Br)3‐NH2was performed using PdO as the catalyst to yield [3H]CCK4with a specific activity of 35 Ci

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270404

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractA new method is reported for the synthesis of tri‐18O substituted phosphate monoesters where the phosphoryl oxygen ester bond is16O. The method relies on the reactivity of trivalent phosphorus toward hydrolysis and oxidation to produce dimethyl [18O3]‐phosphorochloridate with a minimal excess of labeled water. This chlorophosphate diester can be used to prepare a wide variety of phosphate monoesters where the three peripherial oxygens are labe

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270405

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractRadioiodination ofp‐(trimethylstannyl)penicillin V with [125I]Na using a modification of the chloramine‐T method is simple, high yielding, and site‐specific. The structure and penicillin binding protein (PBP) affinity ofp‐[125l]‐penicillin V (IPV) are similar to penicillin G and the product can be used directly without purification in the PBP assay. Because of the high degree of stability toward autoradiolysis and equivalent PBP binding affinity, IPV can be used in place of [3H]‐penicillin G or [14C]‐penicillin G for thes

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270406

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractAn efficient two‐step synthesis of 8‐chloro‐1‐methyl‐6‐phenyl‐[3H]‐S‐triazolo‐[4,3‐a][1,4]‐benzodiazepine (alprazolam) and 8‐chloro‐6‐(2‐chlorophenyl)‐1‐methyl‐[3H]‐S‐triazolo‐[4,3‐a][1,4]‐benzodiazepine (triazolam) labelled with carbon‐13 or carbon‐14 from their corresponding hydrazines is reported. The method involves acylation of the appropriate hydrazine using the mixed carbonic anhydride of sodium [13C] or [14C] acetate and isobutylchloroformate under mild conditions. Thermolysis of the resulting acetylhydrazides gave the target carbon

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270407

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

Abstract14C‐labelled 2‐[4‐(p‐fluorobenzoyl)piperidin‐1‐yl]‐2′‐acetonaphthone hydrochloride (4), a glutamate release inhibitor for studying the pharmacokinetic profiles of E‐2001, was synthesized in two steps using 2‐bromo‐2′‐[carbonyl‐14C]‐acetonaphthone (1) as

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270408

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractA short, efficient synthesis for 1‐(2‐[18O2]‐nitro‐1‐imidazolyl)‐3‐methoxy‐2‐propanol ([18O2]‐misonidazole) from 2‐aminoimidazole is described. The required18O‐labeled sodium nitrite (82.6 atom %) was conveiently synthesized by the treatment of sodium nitrite with DOWEX 50W (H+) in H218O. When 2‐aminoimidazole reacted with excess of18O‐labeled sodium nitrite in the presence of sulfuric acid containing copper sulfate in H218O, the18O‐labeled 2‐nitroimidazole was formed with a reasonable yield (43%). [18O2]‐Misonidazole (70 atom %) was achieved with good yield by the coupling of sublimed18O‐labeled 2‐nitroimidazole with freshly distilled 1,2‐epoxy‐3‐methoxypropane in ethanol in the presence of a catalytic amount of anhydrous potassium carbonate under reflux for one hour. The desired product was purified by recrystalization and TLC, and characterized by1H NMR and mass spectra. The18O content and distribution of synthetic18O‐labeled misoni

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270409

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

Abstract[33P] Potassium peroxydiphosphate (PDP) was prepared by the electrochemical oxidation of [33P] orthophosphate in alkaline solution. After purification by repeated crystallization from aqueous methanol, the radiochemical purity of the final product was 96.5% [33P] PDP and 3.5% [33P] orthophosphate. Overall radiochemical yield was 81%; electrochemical yield was 40%.

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270410

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractNovel or improved synthesis of six deuterated 1‐alkenes (1‐hexene‐[3,3‐2H2], 5‐methyl‐1‐hexene‐[3,3‐2H2], 1‐pentene‐[1,1,2‐2H3], 1‐hexene‐ [2‐2H], 1‐hexene‐[1,1,3,3‐2H4] and 1‐hexene‐[1,1,2,3,3‐2H5]) are reported. The isotopic purities of these labelled alkenes were

ISSN:0362-4803    

DOI:10.1002/jlcr.2580270411

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY