Yamashita, Junichi published the artcileStudies on antitumor agents. V. Syntheses and antitumor activities of 5-fluorouracil derivatives, SDS of cas: 56177-80-1, the main research area is uracil fluoro derivative preparation antitumor; fluorouracil derivative preparation antitumor.
Six types of 5-fluorouracil (5-FU) derivatives were synthesized; namely, 2,4-di-O-substituted, 2-O-substituted, 4-O-substituted, 1,3-disubstituted, 1-substituted and 3-substituted compounds Thus, 2,4-dichloro-5-fluoropyrimidine was treated with BuONa in BuOH to give 2,4-dibutoxy-5-fluoropyrimidine. After oral administration of these compounds to rats, the blood levels of 5-FU were determined Among O-substituted derivatives, a 4-O-substituted derivative was most easily activated to 5-FU and 2-O-substituted derivatives were next most easily activated. Among N-substituted derivatives, acyl and sulfonyl derivatives showed the highest 5-FU releasing abilities and 1-alkoxymethyl substituted derivatives showed low ability. N-Alkyl substituted derivatives were not activated to 5-FU. Several compounds which gave higher blood levels of 5-FU than that obtained with 1-(tetrahydro-2-furyl)-5-fluorouracil (Thf-FU), as well as same related compounds, were selected and their antitumor activities were examined The 2-O-substituted derivatives, 2-butoxy-5-fluoro-4(1H)-pyrimidone and 2-benzyloxy-5-fluoro-4(1H)-pyrimidone, were as effective as Thf-FU. The activities of 2,4-di-O-substituted derivatives, 2,4-dibutoxy-5-fluoropyrimidine and 2,4-dibenzyloxy-5-fluoropyrimidine, against Ehrlich carcinoma and against sarcoma 180, resp., were the same as those of Thf-FU. The 1-substituted derivatives, 1-ethoxymethyl-5-fluorouracil and 1-(1-ethoxy-1-phenylmethyl)-5-fluorouracil, were found to be as effective as Thf-FU.
Chemical & Pharmaceutical Bulletin published new progress about Antitumor agents. 56177-80-1 belongs to class pyrimidines, name is 2-Ethoxy-5-fluoropyrimidin-4(3H)-one, and the molecular formula is C6H7FN2O2, SDS of cas: 56177-80-1.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia