摘要:

AbstractThe synthesis of betaxolol, a new β‐blocking agent, labelled with tritium in high specific activity (49 Ci/mmol) is described. The tritium was incorporated into the molecule via a catalytic reductive debromination of the 2,6‐dibromobetaxolol precursor in the presence of tritium gas. This labelled compound has been used in receptor binding studies and also in studying the release of betaxolol from rat atrial slices on electrical stimula

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250902

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

Abstract1,4‐Diazabicyclo[2,2,2]octane (DABCO) is an efficient quencher of singlet oxygen, O2(1Δg), and is used as an indicator of O2(1Δg) intermediacy in both chemical and biochemical oxidative processes. The quenching is physical in character and the fully deuteriated derivative, DABCO‐2H12, is a molecule of potential mechanistic importance. Its synthesis with>98% isotopic purity is desc

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250903

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractIminodiacetic acid derivatives of meta amino hippuric acid (MAHIDA) and ortho amino hippuric acid (OAHIDA) have been synthesized in the course of our continuing investigation of99mTc‐labeled hippuric acid analogs for application for renal function measurements. The two derivatives yielded stable99mTc complexes using Sn(II) reduction method and are excreted rapidly via the GU tract as shown in animal biodistribution studies. Clearance of these two complexes is lower than that of the analog formed with para amino hippuric acid (PAHIDA) previously reported. Some aspects of structure activity relationship associated with PAHIDA point to the fact that para derivative has optimal renal excretory characteristic

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250904

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe easy preparation of 2‐bromo [1‐3H] ethanol allows the tritium labelling of molecules bearing S‐ or N‐ hydroxyethyl groups. Thus S‐(2‐hydroxy [2‐3H] ethyl) glutathione and [3M]‐Melphalan were synthesised with specific radioactivities of around 10 mCi/mmol (370 MBq/mmol). These values could be theoretically raised to 10 Ci/mmol (370 GBq/mmol), according to the specific activity of the labelling precursor, sodium [

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250905

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractA method for tritiation of 2‐azido‐N(6)‐benzyladenine (AZBA), a photoaffinity analog of the plant hormone N(6)‐benzyladenine (BA), was developed. The synthetic sequence involves condensation of 2,6‐dichloropurine with m‐iodobenzylamine to yield 2‐chloro‐N(6)‐m‐iodobenzyladenine, followed by selective hydrodeiodination with tritium gas over palladium catalyst in pyridine solution to give 2‐chloro‐N(6)‐m‐tritiobenzyladenine. The known conversion of this compound to AZBA enables preparation of the photoaffinity label compound with specific activity high enough to permit detection of cytokinin‐binding proteins existing at low co

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250906

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe title compound was prepared by direct radiochemical synthesis from 2‐acetylamino‐9‐[(2‐hydroxyethoxy)methyl]‐9H‐purine. The product had a specific activity of 21.5 Ci mmol−1and a radiochemical purity of 99.2%. The general approach described may be applicable to other “acycl

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250907

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractSyntheses of the title compounds from diethyl succinate and from dimethyl acetylenedicarboxylate in 16% and 18% overall yield, respectively, are described; a procedure for converting these specifically deuterated diamines into the corresponding bis(ammonium nitrate) salts in 62% and 60% yield, respectively, is presented.

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250908

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe usefulness of immunoaffinity methods for the preparation of biologically fully active radiolabelled antibodies was investigated, using anti‐β‐chorionic gonadotropin as a model substance. Immunoaffinity purification increased the fraction of antigen binding antibody after previous labelling from 25 % to 81 %. Radiolabelling of anti‐β‐chorionic gonadotropin while bound to the antigen resulted in biologically highly active material, possibly due to the protection of the immunologically active sites on the antibody during the labelling procedure. Immunoaffinity purification prior to labelling did not result in biologically active material. Elution yields from immunoaffinity supports were gene

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250909

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

Abstract14C‐ and35S‐labelled 2‐mercaptobenzimidazole and 1‐methyl‐2‐mercaptobenzimidazole were synthesized from14C‐carbon disulfide,35S‐thiourea,14C‐methyl iodide and35S‐thiourea, respectively, for use in studies on the mechanism of action of antithyroid drugs. The products were purified by chromatography on silica and isolated with radiochemical purities of greater than 98%, yields of 45‐77% and specific activities

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250910

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY

摘要:

AbstractThe synthesis of [14C]‐labeled bromobenzene, 2‐bromophenol, 4‐bromophenol, 1,2‐dibromobenzene, 2‐bromobenzonitrile, 2‐bromotoluene, and 2‐bromoanisole are reported. [14C]‐Aniline is selectively monobrominated to ortho‐and para‐bromoanilines in 5 to 3 ratio. The separated bromoanilines are diazotized and either reduced, hydrolyzed, coupled to bromide, coupled to cyanide, or coupled to carbon. 2‐Bromophenol is O‐methy

ISSN:0362-4803    

DOI:10.1002/jlcr.2580250911

出版商:John Wiley&Sons, Ltd.    

年代:1988

数据来源: WILEY