摘要:

Abstract3‐[4‐]4‐(3‐Methylphenyl)‐1‐piperazinyl[butyl]‐2,4‐imidazolinedione, CI‐926 (1), and 3‐[4‐4‐(3‐ethoxyphenyl)‐1‐piperazinyl]butylamino‐5,5‐dimethyl‐2‐cyclohexen‐1‐one, CI‐927 (2) are new antihypertensive agents which have been carbon‐14 labeled in three steps starting from ethylene‐14C2oxide (5). The overall radiochemical yields for1and2were 69% and 66% respectively. The specific activity for both compounds wa

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240402

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractA synthetic procedure for 1,3‐di(trideuteromethyl)uric acid is described. Deuterium labeling of the N‐1 and N‐3 positions was achieved by methylation of 4‐amino‐5‐carbethoxyuracil with di(trideuteromethyl)‐sulfate followed by cyclization of the dimethylated intermediate by heating. The synthesis resulted in a product with 99.4% d6isotopic purity, which is selectively deuterated in the methyl groups at the N‐1 and N‐3 positions an

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240403

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractThe synthesis of six regiospecific deuterated D,L‐homoserine lactone hydrochlorides from the appropriately deuterated 2‐bromo‐1‐(tetrahydropyranyloxy) ethanes which were obtained by reduction of the corresponding ethyl bromoacetates are described. The proton nmr of each lactone is recorded and the chemical shift and coupling constants are r

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240404

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

Abstract[thienyl‐3‐14C]Temocillin has been prepared from [1‐14C]chloroacetic acid via 3‐[3‐14C]thienylmal

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240405

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractTwo amino acids,t‐BOC‐O‐ethyl‐D‐tyrosine andt‐BOC‐phenylalanine, have been synthesized in tritium labeled form via exchange with tritium gas over catalyst on an unlabeled precursor and dehydrohalogenation on an iodinated precursor respectively. The tyrosine derivative has been obtained in specific activities of 4 ‐ 7 Ci/mmol; tritium NMR indicates that at least 80% of the tritium resides in the benzylic position of the molecule. The phenylalanine has been synthesized with a specific activity of greater than 35 Ci/mmol. Tritium NMR confirms specific tritium/iodine replacement

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240406

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractTritium labeled Conduritol B epoxide was prepared by a six step synthesis, starting with p‐benzoquinone. The tritium was introduced into the molecule in the second step by reducing the quinone with sodium boro3H hydrid

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240407

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractThe four14C‐labelled stereoisomers of both 3‐(2,2‐dichloroethenyl)‐2,2‐dimethylcyclopropanecarboxylic acid and 3‐(2,2‐dibromoethenyl)‐2,2‐dimethylcyclopropanecarboxylic acid, the improtant acid components of various potent insecticidal pyrethroids, were prepared efficiently from [1‐14C]chrysanthemic acid (5) for use in comparative metabolic studies. α‐Bromo‐β‐naphthyld,l‐cis, trans‐[1‐14C]chrysanthemate (6) was oxidized with osmium tetroxide‐sodium periodate to give the formyl ester (7) in 78% yield. Wittig reaction of7with dichloromethylenetris(dimethylamino)phosphorane at −75 ‐ −70 °C afforded the dichlorovinylated ester (8) quantitatively. Optical resolution of8by preparative HPLC using a chiral‐phase column led to the four stereoisomers (8a‐8d) with optical purities more than 99%. Hydrolyses of the esters (8a‐8d) yielded the corresponding optically active 3‐(2,2‐dichloroethenyl)‐2,2‐dimethyl [1‐14C]cyclopropanecarboxylic acids (1a‐1d) quantitatively. Similarly, Wittig reaction of the formyl ester (7) with dibromomethylenetris(dimethylamino)phosphorane, followed by optical resolution and hydrolysis, gave four optically active 3‐(2,2‐dibromoethenyl)‐2,2‐dimethyl [1

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240408

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractFor additional pharmacokinetic and metabolism studies in laboratory animals and in humans, Go 10213 was labelled with carbon‐14 located on the carbonyl carbon atom of the ethyleneurea ring (Ring B) of the molecule. [imidazolidinone‐2‐14C]Go 10213 having a specific activity of 6.06 μCi/mg (1.75 mCi/mmol) was synthesised starting with [14C]ethyleneurea in two

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240409

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

AbstractThree syntheses of radiolabelled 2‐[2‐(2‐N,N‐Dimethylaminomethyl‐5‐furanyl‐methylthio)ethylamino]‐5‐(6‐hydroxy‐4‐picolyl)‐4‐pyrimidone trihydrochloride (donetidine trihydrochloride) are described. One describes the preparation of the free base, and two of its trihydrochloride.1. A five stage synthesis (Scheme 1) which gave14C‐donetidine (8) labelled in the C2position of the pyrimidone ring starting from barium [14C]cyanamide. The overall radiochemical yield for the synthesis was 9% to give (8) at a specific activity of 57.8mCi/mmol.2. A three stage synthesis (Scheme 2) which gave14C2‐donetidine trihydrochloride (14) labelled in both methylenes of the aminoethylthio moiety starting from [1,2‐14C2]‐cysteamine hydrochloride. The overall radiochemical yield for the synthesis was 18% to give (14) at a specific activity of 15.4mCi/mmol.3. A five stage synthesis (Scheme 3) which gave3H‐donetidine trihydrochloride (22) labelled in the methylene of the furanlmethylthio moiety starting from sodium boro[3H]‐hydride. The overall radiochemical yield for the synthesis was 1% to give (22)

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240410

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY

摘要:

Abstract6,7‐dimethoxy‐4 (parachlorobenzyl) (D‐3) isoquinoline :6and 6,7‐dimethoxy‐4 [parachlorobenzyl (methylene14C)] isoquinoline:11were prepared respectively by the condensation of α‐deuterio‐veratrylaminoacetaldehyde diethylacetal :4withparachlorobenzaldehyde and the reaction ofparachlorobenzaldehyde (carbonyl14C) :9with veratrylaminoacetaldehyde

ISSN:0362-4803    

DOI:10.1002/jlcr.2580240411

出版商:John Wiley&Sons, Ltd.    

年代:1987

数据来源: WILEY