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Autor: Donald G. Walker, Robert T. Standridge, J. E. Swigor

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 36:479-492

Reductive cleavage of the C13 side chain of paclitaxel (3) followed by regioselective silylation gave 7-triethylsilylbaccatin III (6). Successive reaction of L-threonine methyl ester hydrochloride (7) with tert-butoxydiphenylchlorosilane, benzaldehyd

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4a433cdfe4464fb02f47918067a7e4e2
https://doi.org/10.1002/jlcr.2580360512

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Synthesis of carbon-14 labeled Taxol® (paclitaxel)

Autor: J. E. Swigor, Daniel R. Schroeder, Joydeep Kant, Donald G. Walker

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 34:973-980

Reductive cleavage of the C13 side chain of Taxol® (1, paclitaxel) followed by regioselective silylation gave 7-triethylsilylbaccatin III (4). 3-O-Triethylsilylation of 5 and subsequent reaction with benzoyl chloride-C7-14C gave azetidinone 7. Coupl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::dd8a1d797ba2ae93a843ffe21fea418d
https://doi.org/10.1002/jlcr.2580341010

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Synthesis of 5-fluoro-3-[3-[4-(2-[14C]-5-methoxy-4-pyrimidinyl)-1piperazinyljpropypiperazinyl]propyl]-1H-indole dihydrochloride

Autor: U. J. Haynes, J. E. Swigor

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 34:101-106

The synthesis of 5-Fluoro-3-[3-[4-(2-[14C]-5-methoxy-4-pyrimi-dinyl)-1-piperazinyl]propyl]-1H-indole dihydrochloride (5) was achieved by coupling [14C] formamidine acetate (1) and dimethylmethoxymalonate in methanol containing sodium methoxide at 60�

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https://doi.org/10.1002/jlcr.2580340114

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Synthesis of 2E, 4E, 8E - nonatetraenoic acid-3, 7-dimethyl-1-[14C]-9-(2′, 6′, 6′-trimethylcyclohex-1-enyl)-4-(N-acetamino) phenylester

Autor: J. E. Swigor, U. J. Haynes

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 33:991-994

The title compound 4-(N-acetylamino) phenyl-1-[14C] retinoate (3) was synthesized by a 2-step sequence. Carboxyl-[14C] vitamin A (1) was treated with ethylchloroformate to form the mixed anhydride (2). Treatment with acetamidophenol and heating with

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https://doi.org/10.1002/jlcr.2580331014

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Synthesis of 7-[α-(2-amino-[2-14C]thiazol-4-yl)-α-(Z)-methoxyiminoacetamido]-3-(1-methylpyrrolidinio)methyl-3-cephem-4-carboxylate hydrochloride ([14C]cefepime hydrochloride)

Autor: J. E. Swigor, Robert T. Standridge

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 33:759-765

The title compound 9 was prepared by the route outlined in Scheme I. [14C]Thiourea (1) was condensed with ethyl 4-bromo-3-oxo-2-methoxyiminoacetate (2), providing ethyl 2-(2-amino-4-[2-14C]thiazolyl)-2-methoxyiminoacetate (3), as the pure Z-isomer. S

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https://doi.org/10.1002/jlcr.2580330812

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Syntheses of 9-(2′-monoethylphosphonomethoxyethyl)-8-[14C]guanine ([14C]-EPMG) and 9-(2′-phosphonomethoxyethyl)-8-[14C]guanine ([14C]-PMEG)

Autor: J. E. Swigor, U. J. Haynes

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 33:795-799

The synthesis of the title compounds [14C]-PMEG (5) and [14c]-EPMG (6) are described. Treatment of [14C]guanine with acetic anhydride in 1-methyl-2-pyrrolidinone gave [14C]N-acetylguanine (2). Reaction with 2-(diethylphosphonomethoxy) ethylmethanesul

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a17cd233690c9f6e503f03429b1ed0e2
https://doi.org/10.1002/jlcr.2580330816

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Synthesis of Carbon-14 labeled gadoteridol, [1,4,7-Tris(carboxymethyl)-10-(2-hydroxy-1-[14C]propyl)-1,4,7,10-tetraazacyclododecanato]gadolinium

Autor: J. E. Swigor, Douglas D. Dischino

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 31:455-458

Carbon-14 labeled Gadoteridol, [1,4,7-Tris(carboxymethyl)-10-(2-hydroxy-1-[14C]propyl)-1,4,7,10-tetraazacyclododecanato]gadolinium, was prepared from 1-[14C] propylene oxide in a total yield of 30.4% and a radiochemical purity of 99.2%.

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https://doi.org/10.1002/jlcr.2580310605

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Synthesis of (S)-1-[3-hydroxy-2-(phosphonylmethoxy) propyl]-[2-14C]cytosine ((S)-[14C] HPMPC)

Autor: J. E. Swigor, U. J. Haynes, J. J. Bronson

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 29:1217-1221

The synthesis of (S)-[14C]HPMPC (4) is described. Heating [2-14C]cytosine (1) in N, N-dimethylformamide with (R)-3-0-benzyl-2-0-[(diethylphosphonyl)methyl]-1-0-(methylsulfonyl) glycerol in the presence of cesium carbonate gave (S)-1-[3-benzyloxy-2-(d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8e0721aee84a3ee6b6689abd26e0f56d
https://doi.org/10.1002/jlcr.2580291106

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Synthesis of 4-amino-5-chloro-N[2-(diethylamino)ethyl]-2- [(butan-2-on-3-yl)oxy]-[carbonyl-14C]benzamide hydrochloride (14C-batanopride)

Autor: J. E. Swigor, Robert T. Standridge

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 29:983-988

The title compound (1) was synthesized by a 7-step sequence. 4-Amino-2-hydroxy-[carbonyl-14C]benzoic acid (1) was selectively methylated to provide the ether ester 2, which was smoothly chlorinated in acetic acid to give 3. The ester was hydrolyzed w

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https://doi.org/10.1002/jlcr.2580290902

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Synthesis of (±)-trans-6-[4,4-bis(4-fluorophenyl)-3- (1-methyl-1H-tetrazol-5-YL)-1(E),3-[2-14C] butadienyl]-4-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one

Autor: George M. Luke, J. E. Swigor

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 29:193-199

A convergent synthesis of the title compound (BMY-22089) is described. [14C]Methyl iodide was used to alkylate 1,5-dimethyltetrazole which was added to 4,4′-difluorobenzophenone to give the tertiary alcohol 4. Dehydration gave, the olefin 5 which w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::14374300860f1467b8609c061934674a
https://doi.org/10.1002/jlcr.2580290209

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