5-Fluorouracil Derivatives. X
With the aim of diminishing the toxicity of 5-fluorouracil (1) and obtaining biologically active derivatives of 1 suitable for oral administration, α-alkoxyalkyl groups were introduced at the 1-, 3-and 1, 3-positions of 1. Alkoxyalkylation can be effected by four methods : (i) reaction of 1-alkoxyal...
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| Veröffentlicht in: | Chemical & pharmaceutical bulletin 1986-01, Vol.34 (1), p.150 |
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| creator | OZAKI, SHOICHIRO WATANABE, YUTAKA HOSHIKO, TOMONORI NAGASE, TOSHIO OGASAWARA, TOMIO FURUKAWA, HIROYUKI UEMURA, ATSUHIKO ISHIKAWA, KATSUTOSHI MORI, HARUKI HOSHI, AKIO IIGO, MASAAKI TOKUZEN, REIKO |
| description | With the aim of diminishing the toxicity of 5-fluorouracil (1) and obtaining biologically active derivatives of 1 suitable for oral administration, α-alkoxyalkyl groups were introduced at the 1-, 3-and 1, 3-positions of 1. Alkoxyalkylation can be effected by four methods : (i) reaction of 1-alkoxyalkyl chloride (2) with 1, (ii) reaction of acetal with 2, 4-bis (trimethylsiloxy)-5-fluoropy-rimidine, (iii) addition reaction of α-unsaturated ether with 1, (iv) aminolysis of 1-alkylthio-carbonyl-3-(1-alkoxyalkyl)-5-fluorouracil. The toxicity of the products was less than that of 1, and some of these compounds showed moderate antitumor activity against L-1210 leukemia. |
| format | Article |
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| ispartof | Chemical & pharmaceutical bulletin, 1986-01, Vol.34 (1), p.150 |
| issn | 0009-2363 1347-5223 |
| language | eng |
| recordid | cdi_proquest_journals_1460088066 |
| source | J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| title | 5-Fluorouracil Derivatives. X |
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