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1. |
Improved conventional synthesis for14C‐labeled polyglutamates of folic acid |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 737-751
Catherine R. Ferenz,
David Y. Graham,
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摘要:
AbstractThe majority of folates existing in nature are of the pteroylpolyglutamyl form and are unable to supportLactobacillus caseigrowth until the δ‐linked glutamyls are digested by conjugase enzymes. Most studies involving folate absorption have utilized monoglutamyl forms of folate, primarily folic acid. Synthetic pteroylpolyglutamates prepared by solid phase or conventional synthesis provided conjugated materials with which to study the absorption and metabolism of natural derivatives; however, the synthetic hepataglutamates support microbiological growth prior to enzymatic hydrolysis where as the natural conjugates do not. Incomplete purification of intermediate peptides during the synthesis would be the most likely explanation of this growth phenomenon. A modified solution synthesis has been developed which improves upon intermediate peptide condensations, increases product yields, and provides a heptapeptide which does not support microbiological growth until after enzymatic hydrolys
ISSN:0362-4803
DOI:10.1002/jlcr.2580270702
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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2. |
124Sn‐labelled tetra‐n‐butyltin and tri‐n‐butyltin bromide |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 753-761
J. P. Testa,
C. A. Dooley,
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摘要:
AbstractStable isotope‐labelled tetra‐n‐butyl (124) tin was synthesized by the reaction of n‐butylmagnesium bromide with124SnCl4. Tri‐n‐butyltin bromide was synthesized by bromine cleavage of the tetraalkyltin. The compound can be used to trace chemical, biological and physical processes in environmental and metabolic studies using gas chromatography and electron impact low resolution mass spectrometry. The simplified spectra of the isotopically enriched compounds leads to a twofold increase in detection sensitivi
ISSN:0362-4803
DOI:10.1002/jlcr.2580270703
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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3. |
Improved yields in the synthesis of 4‐nitro[1‐13C]aniline |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 763-766
Ibrahim Yilmaz (1),
Henry J. Shine,
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摘要:
Abstract4‐Nitro[1‐13C]aniline has been prepared in overall yield of 54%, based on labeled acetone, by modification of a standard procedure
ISSN:0362-4803
DOI:10.1002/jlcr.2580270704
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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4. |
A new and efficient synthesis of monotritiomethyl iodide |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 767-776
Manouchehr Saljoughian,
Hiromi Morimoto,
Albert M. Dorsky,
Henry Rapoport,
Hendrik Andres,
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摘要:
AbstractA new and efficient synthesis of high specific activity TCH2I containing one atom of tritium per molecule is reported. The precursors for this reagent, chloromethyl p‐phenylbenzoate or bis‐chloromethyl terephthalate, were prepared by the condensation of the corresponding acid chlorides with paraformaldehyde in the presence of zinc chloride. Tritiodehalogenation of the precursors with tritium gas and Pd‐C (10%) in dimethylformamide afforded the desired tritioesters. Cleavage of the esters by lithium iodide at 180°C (SN2type reaction), or by HI at 140°C gave mono tritium labeled methyl iodide in more than 95% yield. The reaction of the latter with a number of amines yielded tritium labeled N‐methylated products readily as was shown by Radio‐HPLC. The specificity of the labeling in the final products was confirmed by tritium nmr s
ISSN:0362-4803
DOI:10.1002/jlcr.2580270705
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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5. |
The synthesis of 2‐14C‐N‐nitrosothiazolidine |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 777-781
David W. Cragin,
Takayuki Shibamoto,
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摘要:
Abstract2‐14C‐N‐Nitrosothiazolidine was synthesized with a chemical purity of 99.6%, a radio chemical purity of 99.4%, and an overall yield of 30.7%. Unlabelled N‐nitroso‐thiazolidine, synthesized using the same method, resulted in a purity of 99.85% by capillary GC and 99.7% by HPLC. Analysis of N‐nitrosothiazolidine by GC was found to require a low injection port temperature of 160°C to prevent denitrosation in the injection port. During the nitrosation of thiazolidine, if the pH was reduced below 4 with hydrochloric acid, ring hydrolysis occurred, and chlorinated disulfide comp
ISSN:0362-4803
DOI:10.1002/jlcr.2580270706
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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6. |
Synthesis of deuterated β‐carotene |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 783-788
H. Robert Bergen,
James A. Olson,
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摘要:
AbstractThe synthesis of 10,10′,19,19,19,19′,19′,19′‐2H8‐β‐carotene is described. The double condensation (C15+C10+C15=C40) of the Wittig salt of 9,9,9,10‐2H4‐β‐ionylidene ethanol with the symmetrical C10dial 2,7‐dimethyl‐2,4,6‐octatrienedial led directly to2H8‐β‐carotene. The symmetrical labelling pattern of this deuterated β‐carotene will function as a tracer for the study
ISSN:0362-4803
DOI:10.1002/jlcr.2580270707
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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7. |
Optimized synthesis of radioiodinated rhodamine‐123 |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 789-802
Manhar M. Vora,
Richard M. Lambrecht,
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摘要:
AbstractRhodamine‐123 (Rh123) was iodinated with123I in presence of Iodogen. Yield of the labelled Rh123 varied greatly depending upon various reaction parameters. Optimum reaction conditions with respect to molarity and pH of the buffer, reaction time, amounts of iodogen, carrier iodide and Rh123, were determined through carefully controlled reactions. Radiochemical yields of 50–60% were obtained within less than 2 hrs. using 0.05M NH4H2PO4buffer at pH5, 200 μg iodogen, 250 μg Rh123 and no‐carrier‐added iodide. Separation of the labelled Rh123 in greater than 98% radiochemical purity was achieved by flash chromatography on silica gel. The overall isolated yield of radioiodinated Rh123 ranged from 25–35% with respect to the added radioiodide. TLC and HPLC methods were developed for analysis of the labell
ISSN:0362-4803
DOI:10.1002/jlcr.2580270708
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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8. |
Use of kinetic isotope effects in enzymatic oxidation of D‐[6‐3H]galactose for increasing its molar activity |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 803-810
G. P. Akulov,
N. A. Korsakova,
B. K. Kudelin,
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摘要:
AbstractLarge kinetic isotope effects have been observed in D‐[6‐3H]galactose enzymatic oxidation reactions catalyzed by the galactoseoxidase. It is possible to use these effects for considerable increase of the molar activity of D‐galactose labelled with tritium in the posit
ISSN:0362-4803
DOI:10.1002/jlcr.2580270709
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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9. |
Synthesis of D3‐sulpiride and its (R) and (S) isomers |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 811-821
M. Al‐koutayni‐rifai,
G. Jamet,
R. R. Kerr,
L. Jung,
J. C. Koffel,
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摘要:
AbstractRacemic d3‐sulpiride, (R)‐(+)‐d3‐sulpiride and (S)‐(−)‐d3‐sulpiride (with three deuterium atoms in the methoxy function ortho to the benzamide), as well as (R)‐(+)‐sulpiride and (S)(−)‐sulpiride were synthesized. The structures were characterized by melting points, IR,1H‐NMR, GC‐MS and polarimetry. The measu
ISSN:0362-4803
DOI:10.1002/jlcr.2580270710
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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10. |
Aryltrimethylammonium trifluoromethanesulfonates as precursors to aryl [18F]fluorides: Improved synthesis of [18F]GBR‐13119 |
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Journal of Labelled Compounds and Radiopharmaceuticals,
Volume 27,
Issue 7,
1989,
Page 823-833
Michael S. Haka,
Michael R. Kilbourn,
G. Leonard Watkins,
Steven A. Toorongian,
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摘要:
AbstractAromatic nucleophilic substitution of various trimethylammonium trifluoromethanesulfonates with [18F]fluoride has been evaluated. Fluorinations were studied over a temperature range of 45–165°C, with decay corrected yields ranging from 20–80%. [18F]GBR 13119, 1‐[2‐{(4‐[18F]fluorophenyl)(phenyl)methoxy}ethyl]‐4‐(3‐phenylpropyl)piperazine, a potential radio‐tracer for the dopamine uptake system, has been prepared in no‐carrier‐added form from 4‐N,N,N,‐trimethylaniliniumphenylmethanone trifluoromethanesulfonate. Purification by solid‐phase techniques yielded the product in 20% decay corrected radiochemical yield and>98% radiochemical and
ISSN:0362-4803
DOI:10.1002/jlcr.2580270711
出版商:John Wiley&Sons, Ltd.
年代:1989
数据来源: WILEY
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