| abstract |
PURPOSE: To obtain the titled compound useful as an intermediate for synthesizing daunomycin, etc. by a simple reaction operation in high yield, by treating a specific naphthol derivative as a raw material in an acidic aqueous solution in the presence of a divalent mercuric ion. n CONSTITUTION: A 2-(2-trialkylsilylethynyl)-1,2,3,4-tetrahydro-2-naphtol derivative shown by the formula I [R 1 and R 4 are H, OH, or alkoxy; R 2 and R 3 are H or linked to form group shown by the formula II (X 1 and X 2 are R 1 , R 4 , lower alkyl, etc.); R 5 WR 7 are lower alkyl] is treated in an acidic aqueous solution in the presence of a mercuric ion such as mercuric oxide, etc. at room temperature for ≤ tens hours, to give the aimed compound shown by the formula III. The acidic aqueous solution is prepared from a mixed solution of an aqueous solution of a mineral acid such as 7W10 normal sulfuric acid, etc., an organic solvent, and water. n USE: An intermediate for synthesizing daunomycin, etc. that are an aglycone of anthracycline which is an aminoglycosdie antibiotic showing carcinostatic activity. n COPYRIGHT: (C)1986,JPO&Japio |