abstract |
NEW MATERIAL:3-(N-Formyl-N-hydroxyamino)-2(R)-hydroxypropylphonic acid of formula I and its salts. n USE: A preventive and a remedy for bacterially infected diseases. n PROCESS: For example, diethyl 2(R), 3-dihydroxyprophylphosphonate is made to react with a reaction reagnet of formula R 2 SO 3 H (R 2 =alkyl or aryl), e.g. p-toluene sulphonic acid chloride, or its reactive derivative. The reaction product obtained is then made to react with an OH-protecting agent and a compound of formula II (R 3-4 are protecting proup of hydroxy and amino groups), e.g. N,O-bis (trimethylsilyl) acetamide to give a compound of formula III (R 5 =H or hdroxy protecting goup), which is successively subjected to the hydrolysis and the formylation to afford the objective compound. n COPYRIGHT: (C)1979,JPO&Japio |