摘要:

AbstractThe synthesis of Asaley labelled with14C in the mustard (Asaley‐must‐14C) or the leucine (Asaley‐leu‐14C) moiety is described. In the former, ethyl pamino‐Nα‐acetyl‐DL‐phenylalanyl‐L‐leucinate was reacted with ethylene oxide(U)‐14C to give the bis(hydroxyethyl)amino analogue, which was converted to Asaley by treatment with thionyl chloride. Asaley labelled in the leucine moiety was prepared by condensation of N‐acetylsarcolysin with ethyl leucinate(U)‐14C in the presence of dicyclohexylcarbodiimide. The identity of the products was established by spectroscopic, chemical, and

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170202

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractThis report describes the synthesis of carbon‐14 labeled 3‐phenylpropoxyguanidine cyclohexylsulfamate from barium [14C]‐carbonate. The product is labeled at the 3‐position of the propyl chain, adjacent to the phen

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170203

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractThymine‐α,α,α‐d3(4) was synthesized from perdeuterated methyl iodide and pyrimidine‐lithium. Thymidine‐α,α,α‐d3(8) was then synthesized by coupling compound4with 1α‐chloro‐2‐deoxy‐3,5‐bis(p‐toluoyl)‐α‐D‐ribofuranosyl chloride in the presence of Friedal‐Crafts catalyst. Thymidine‐α,α,α‐d3(8), a metabolic precursor of deoxyribonucleic acid, has potential application for study of human tissue growth kinetics in vivo using

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170204

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractA simple two step synthetic procedure has been developed for the preparation of deuterated lidocaine. The deuterium was incorporated into the 6′‐methyl group which is a metabolically stable position. The overall yield of the synthetic procedure was 41

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170205

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractThe preparations of guvacine hydrochloride, in which a proton in position 2 (11) and protons in positions 2 and 5 (10) are selectively exchanged by deuterium, and of [2,6‐2H]isoguvacine hydrobromide (14a) are described. The deuterium labelled guvacine salts 10 and 11 were synthesized by triethylamine catalyzed exchange of hydrogen for deuterium in methyl N‐nitroso‐1,2,5,6‐tetrahydropyridine‐3‐carboxylate (3) followed by denitrosation and hydrolysis. Treatment of N‐nitroso‐1,4,5,6‐tetrahydropyridine‐3‐carboxylic acid with methanolic thionyl chloride gave 3,4,5,6‐tetrahydropyridin‐3‐on ketoxime. Compound14awas prepared by sodium borodeuteride reduction of 4‐ethoxycarbonyl‐1‐methylpyridinium iodide (12) followed by N‐demethylation

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170206

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractRFCNU was labelled by14C on three positions.On the carboxyl of the para nitro benzol'c groupOn urea carbonylOn the carbone 1 of the 2, chloro éthyl group

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170207

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

Abstract(U‐14C) Phenol and isobutene under pressure in presence of aluminium phenoxide gave in 60 % yield a mixture of (ring U‐14C) 2‐t‐butylphenol (50 %) and (ring U‐14C)‐2,6‐di‐t‐butylphenol (10 %) which were separated by column chromatography on silicagel. Each t‐butylphenol was nitrated under appropriate conditions to give an 35 % overall yield of (ring‐U‐14C)‐4,6‐dinitro‐2‐t‐butylphenol : specific activity : 27.4 mCi/mMol which was proved by TLC and HPL

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170208

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

Abstract14C labelled phospholipid synthesis through the use of “cyclic enediolpyrophosphate”.Ramirez's phrophosphate1was used in a one pot convenient synthesis of a few [1‐14C]‐acyl phospholipids. Reagent1was condensed with 1,2‐[1‐14C] dipalmitoyl Sn‐glycerol to the cyclic triester phosphate4which without isolation, was reacted with N‐tritylethanolamine, 3‐0‐benzyl Sn‐glycerol and glycerol leading to intermediates5, 6, 7which were deprotected by triethylamine hydrolysis and other a

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170209

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractSpecific methods of tritium labelling onto C‐2 and (or) C‐5 positions of the imidazole ring were successfully applied to thyroliberin (TRF, L‐Glu‐L‐His‐L‐Pro‐NH2).Diazocoupling by diazotized sulphanilic acid and iodination by iodine monochloride of the histidyl residue were chosen to prepare precursors and to quantify the distribution of tritium atoms which were introduced.Catalytic hydrogenolysis in the presence of tritium gas of 5‐iodohistidine2‐ and 2(4‐sulfophenylazo)histidine2‐ derivatives allowed to label these positions with specific radioactivities of 30 Ci and 25 Ci/mmole respectively. For comparison thyroliberin tritiated by direct catalytic exchange is labelled essentially onto C‐2 with a specific rad

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170210

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY

摘要:

AbstractA procedure is described for synthesizing uracil‐1,3‐15N2in 77% yield by the condensation of urea‐15N2with propiolic acid. The uracil‐1,3‐15N2was employed subsequently in a random alkylation with dimethyl sulfate‐d6to give 1‐methyl‐d3‐uracil‐1,3‐15N2, 3‐methyl‐d3‐uracil‐1,3‐15N2, and 1,3‐dimethyl‐d6‐uracil‐1,3‐15N2. Purification of the products resulting from both these reactions was achieved on an ion exchange column. The15N and1H NMR spectra obta

ISSN:0362-4803    

DOI:10.1002/jlcr.2580170211

出版商:John Wiley&Sons, Ltd.    

年代:1980

数据来源: WILEY