摘要:

Abstract1‐Ethyl‐1‐(2‐hydroxyethyl)aziridinium‐1,2‐14C2chloride (1) ([(14C]AF64A), the labelled analogue of a selective presynaptic cholinotoxin, was prepared from labelled ethylene oxide. The synthetic intermediate, 1,2‐14C2‐2[ethyl[2‐[(tetrahydro‐2H‐pyran‐2‐yl)oxy]ethyl]amino]ethanol, obtained in good yield by the reaction of 2‐[(tetrahydro‐2H‐pyran‐2‐yl)oxy]diethylamine with [14C] ethylene oxide, was converted to the corresponding ethyl chloride derivative using CH3SO2Cl/n‐BuLi. Subsequent removal of the THP group under mild acidic condition gave the mono‐armed mustard as a stable hydrochloride salt in an overall chemical yield of 46% and radiochemical yield of 27%. Conversion of the mustard compound to the corresponding az

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271002

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractThis report describes the synthesis of ibuprofen of labeled with carbon‐13 either at the terminal methyl carbons, or at the methine carbon of the isobutyl side chain. The synthetic route involves the removal of the isopropyl group in the isobut I side‐chain of ibuprofen via 2‐[4‐(2‐methyl‐1‐propenyl)phenyl] propionic acid followed by restoration of the isopropyl group with a Wittig reaction, using appropriate carbon‐1 3 labeled acetone as the precursor of the isopropyl group. Interesting NMR coupling data attributable to phosphorous and carbon‐13 are presented in the exp

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271003

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractThis paper describes an application of the pterin synthesis of Taylor and co‐workers for preparation of methotrexate specifically labelled at the N1‐ring nitrogen and at the 4‐amino group with 99 atom percent15N. Oximination of ethyl cyanoacetate‐15N followed by reduction afforded ethyl 2‐aminocyanoacetate‐C15N (3). Condensation with 3‐bromopyruvaldoxime and 4‐methylaminobenzoic acid afforded 2‐amino‐3‐carbethoxy‐5‐N‐methyl‐p‐carboxy‐anilinomethylpyrazine‐1‐oxide‐2‐15NH2(4). Treatment of4awith ammonium hydroxide at room temperature gave the 3‐carboxamide (5a). Reduction of the N‐oxide (PCl3), esterification, and dehydration of the amide (POCl3) afforded the 2‐amino‐3‐cyano‐pyrazine benzoate ester (8). Ring closure with guanidine followed by benzoate ester hydrolysis, glutamate coupling and hydrolysis of the glutamate diester yielded methotrexate‐1‐15N (12a). Amination of the unlabeled 2‐amino‐3‐carbethoxy pyrazine intermediate (4b) with15N‐labelled ammonium hydroxide gave the15N‐carboxamide (5b) which was carried thro

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271004

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractA method for preparation' of in vitro radiocolloidal solution of113mIn (Ca)‐phytate is reported. The radiochemical purity was determined using paper chromatography and it was higher than 95%. Liver uptake in mice was high (87%) with low lung uptake. This radiopharmaceutical has, therefore, medical disgnostic specification

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271005

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractN(isopropyl)‐ and N(isobutyl)‐Iodo‐amphetamine were double labelled with131I and deuterium.The deuterium labelled radiopharmaceuticals showed in mice and rats a higher brain uptake and a lower blood concentration than the controls (injection of the131I‐labelled amphetamine without deuterium). The deuterium effect ist not increasing with higher deuterium content in the radiopharmace

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271006

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractA freeze dried kit formulation for the preparation of99mTc‐[V]‐DMS complex was developed, requiring a single step labeling procedure. Methods of analysis were also developed permitting identification of radiochemical impurities which may be present in radiopharmaceutical solution.99mTc‐[V]‐DMS prepared by the kit method was evaluated in experimental animals and human volunteers. Data demonstrated that the complex formed after kit reconstitution shows tumor seeking properties. Thyroid medullary carcinoma in patients was successfully detected 2 hrs post adminis

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271007

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

Abstract15O‐H2O2is thought to be a candidate of attractive injectable tracers for the study of oxygen metabolism with PET. A simple synthetic method yielding15O‐H2O2in saline solution by the autoxidation of 2‐ethylanthrahydroquinol with gaseous15O‐O2produced by cyclotron target system is de

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271008

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractThe complete chemical synthesis of unsaturated precursors of eicosanoids of series 1,2,3 is described. Selective hydrogenation by gaseous tritium of eicosapolyenoic acid acetylenic analogues was used to introduce the label into dihomo‐α‐linolenic, arachidonic and timnodonic acids, from which [3H]PGE, [3H]PGD and [3H]TXB2were obtained by biosynthesis. From [3H]PGE multiply labelled PGA, PGB, PGFα, PGI2ME, 6‐keto‐PGF1αME were synthesized by chemic

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271009

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractWe have obtained multiple‐tritium‐labelled 5‐α‐androstan‐3‐one, dihydropicrotoxin, dimethyl‐propyl‐3‐chloro‐butyl‐ammonium chloride, 2,2‐di(trifluoromethyl)‐3,3‐dicyanobicyclohept[2,2,1]ane, dihydroalprenolol, undecanoic acid, dihydro‐m,m'‐di‐tert.‐butyl‐p‐coumaric acid and dihydrofusicoccin. By varying the conditions for the hydrogenation of terminal double bonds one can considerably increase the molar radioactivity of such compounds through isotopic exchange. We discuss some tentative explanations of the effect of the labelling reaction conditions upon the synthe

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271010

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY

摘要:

AbstractEnantiomers of metoprolol (1) containing six deuterium atoms in the isopropyl methyl groups [(2R‐2], two deuterium atoms at C‐2 and C‐6 of the aromatic ring [(2S)‐3], and two deuterium atoms at C‐3 of the propanolamine side chain [(2S)‐4] were prepared. Chiral 2,2‐dimethyl‐1,3‐dioxolane‐4‐methanols [(4R)‐5and (4S)‐5] were key synthons. Sources of deuterium were [2H6]‐isopropylamine, 4‐(2‐methoxyethyl)‐2,6‐[2H2]‐phenol (12), prepared by2HCl/2H2O exchange, and (4S)‐2,2‐dimethyl‐1,3‐dioxolane‐4‐[2H2]‐4‐methanol (19), prepared by LiAl2H4reduction of (4S)‐methyl 2,2‐dimethyl‐1,3‐dioxolane‐4‐carboxylate. Enantiomeric excess was greater than 94% for each of the prepared enantiomers, as determined independently by1H NMR spe

ISSN:0362-4803    

DOI:10.1002/jlcr.2580271011

出版商:John Wiley&Sons, Ltd.    

年代:1989

数据来源: WILEY