RESIN-IMMOBILIZED HYDRAZIDE, ITS DERIVATIVE AND SOLID PHASE SYNTHESIS OF PYRAZOLONE

摘要

PROBLEM TO BE SOLVED: To obtain the subject hydrazide useful for the synthesis of pyrazolone capable of using a Mannich reaction according to a solid phase synthetic method by providing the hydrazide with a specific structure. ;SOLUTION: This hydrazide comprises a structure shown by the formula; P-Q-CO-NH-NH₂ [P is a main chain of a resin polymer; and Q is e.g. a (substituted) hydrocarbon side chain]. The hydrazide is obtained by carboxylating a resin polymer (e.g. polystyrene/divinylbenzene copolymer) of the formula; P-QH by e.g. reacting it with n-butyllithium and then with carbon dioxide, obtaining a carboxylic acid resin of the formula; P-Q-CO-OH, esterifying it and reacting a hydrazine (e.g. hydrazine monohydrate) with the thus obtained carboxylate resin in the equivalent ratio of pref. about 0.5 to 5 at pref. 60 to 110°C.;COPYRIGHT: (C)1999,JPO