摘要:

AbstractCis‐diamminedichloroplatinum (II) (cisplatin) is one of the most widely used anticancer drugs today. However, platinum compounds possessing the 1,2‐diaminocyclohexane (DACH) carrier ligand offer advantages over cisplatin with regard to bioavailability, activity and decreased renal toxicity. The trans‐(d,1)‐1,2‐diaminocyclohexane derivatives are the isomeric forms recently chosen by the NCI for large animal studies and phase I/II clinical trials. Here we report the synthesis of four trans‐(d,1)‐1,2‐diaminocyclo‐hexane platinum derivatives labeled with tritium in the cyclohexane ring by catalytic reduction of a cyclohexene precursor with carrier‐free tritiu

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250402

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractTwo methods have been developed for the synthesis of tetradeuterated buspirone. Synthesis of the title compound was accomplished by the reaction of 1‐(2‐pyrimidinyl)piperazine‐3,3,5,5‐d4or 1‐(2‐pyrimidinyl)‐piperazine‐2,2,3,3,‐d4with 8‐(bromobutyl)‐8‐azaspiro[4.5]decane‐7,9‐dion

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250403

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractApparent rate constants (fractional incorporation per minute per mole of organic reactant) were determined for reaction of no‐carrier added F‐18 fluoride with several aliphatic and aromatic substrates in acetonitrile or DMSO. No large differences were seen between tetraethylammonium and potassium Kryptofix‐2,2,2 as supporting cation. Three hexose derivatives with triflate or cyclic sulfate leaving groups all gave apparent rate constants (obtained by dividing fractional incorporation by time in minutes and by molar concentration of reactant) near 0.4 at 23° and 5 at 55°. An aliphatic iodide reacted ten times more slowly. Aromatic substrates tested showed a wide range of rate constants from>50 at 23° (isotope exchange in 2,4‐dinitrofluorobenzene) to 0.6 at 134° (p‐nitro

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250404

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractRadioiodinated long chain aliphatic amines which are substrates of pulmonary monoamine oxidase enzyme system are synthesized for evaluation as potential lung imaging agents. ω‐Phenylhexylamine (48% overall chemical yield) and its β‐methyl substituted analogue (17%) were successfully synthesized from β‐phenylhexanoic acid. γ‐Methyl‐ω‐phenylhexylamine (37%) was prepared from ω‐phenylpentanoic acid. Radioiodination of the phenyl moiety of the amines with no‐carrier‐added [131I]‐NaI was achievedviaa thallium intermediate with 25%, 31% and 36% radiochemical yield respectively in greater than 98% radiochemical purity (calculated specific activity 20 ‐ 40 TBqmmol−1). Thallation of activated aromatic systems proceeded rapidly and in quantitative yields. Isolation of the thallate i

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250405

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractBoth racemic [2‐14C] juvenile hormone III (JH III; methyl‐10,11‐epoxy‐3,7,11‐trimethyl‐2(E),6(E) [2‐14C]dodecadienoate) and its 2‐(Z) isomer were synthesised on a 1 millimolar scale by forming the 9,10 epoxide of geranyl acetone and reacting this with the anion of trimethylphosphono‐[2‐14C]acetate. After purification the yield of [2‐14C] JH III in the radiosynthetic step was 14% (with purity>93% by GC, specific activity 0.4mCi/mmol) and 4.7% (>97%, 0.4mCi/mmol)

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250406

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractSetoperone has been labeled with18F to visualize the serotoninergic receptors by positron emission tomography. The synthesis is carried out by a nucleophilic substitution from a nitro derivative of setoperone with18F−. The synthesis of nitro‐derivative is described as well as the different trials of recovery of ion18F−from neon or aqueous target. The considered technique of labeling allow to obtain from 7.4 GBq (200 mCi)18F, 1.5 to 2 GBq (40–50 mCi) of [18F]setoperone, 110 minutes after the end of bombardment. The specific activity obtained from this quantity of radioactivity is about 37 GBq/μMol (1

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250407

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractA multistep synthetic route to (±)‐10‐[2‐(1‐methyl‐2‐piperidinyl)ethyl]‐2‐methylthio‐10H‐phenothiazine (thioridazine) was developed which allowed for the incorporation of two deuterium atoms in the piperidine ring and a further two in the 1‐position of the ethyl side chain. The key steps involved ruthenium tetroxide oxidation of N‐protected methyl 2‐piperidinylacetate and subsequent lithium aluminum deuteride reduction of 2‐(2‐hydroxyethyl)‐1‐methyl‐6‐piperidinone or the corresponding piperidinoneester. The isotopic purity of the dideuterated and tetrade

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250408

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

Abstract[14C]‐Labeled {[trans‐(8 β)]‐6‐methyl‐1‐(1‐methylethyl)ergoline‐8‐carboxylic acid, 4‐methoxycyclohexyl ester (Z)‐2‐butenedioate (1:1)} (LY281067) (10) was synthesized from unlabeled 6‐methyl‐1‐(1‐methylethyl)ergoline‐8‐carboxylic acid (2). The [14C] label was introduced into the carboxyl group attached to the 8 position of the ergoline nucleus. This site is stable to metabolism. The synthesis involves removal of the unlabeled carboxyl group from 2 and subsequent reinsertion of a [14C]‐labeled carboxyl group into the same position. The radiolabel is not introduced until near the end of the synthesis which allows for ease of

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250409

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250410

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250401

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY