| abstract |
NEW MATERIAL:The pyrazole derivative of formula I (R 1 is H, alkyl, alkylcarboxylic acid residue, its ester, phenyl or benzyl; R 2 is carboxylic acid residue, its ester, carbamoyl, or alkyl; R 3 is alkyl or benzyl). n EXAMPLE: Ethyl 5-[4-(4-chlorobenzyloxy)phenyl]pyrazole-3-carboxylate. n USE: A drug having lipid-level lowering activity. It remarkably increases the HDL- cholesterol level, and has low toxicity. n PREPARATION: The compound of formula I wherein R 2 is CO 2 C 2 H 5 , i.e. the compound of formula III can be prepared e.g. by alkylating or benzylating acetophenone in DMF in the presence of potassium carbonate, subjecting the reaction product to Claisen condensation with diethyl oxalate in the presence of an alkali, and heating and refluxing the resultant enolate sodium salt of formula IIin acetic acid in the presence of hydrazine. n COPYRIGHT: (C)1986,JPO&Japio |