NEW 2-AMINO-2-ETHYNYLMALONIC ESTER DERIVATIVE

PURPOSE:To provide a new 2-amino-2-ethynylamalonic ester derivative, a new ynamide derivative, and a 3-alkylthio-2-amino-butenoic acid derivative, each useful as a vitamin B6 dependent enzyme inhibitor, antibacterial agent or antimycotic agent. CONSTITUTION:The 2-amino-2-ethylmalonic ester of formul...

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Hauptverfasser: NAGAO YOSHIMITSU, KIN KEN
Format: Patent
Sprache:eng
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Zusammenfassung:PURPOSE:To provide a new 2-amino-2-ethynylamalonic ester derivative, a new ynamide derivative, and a 3-alkylthio-2-amino-butenoic acid derivative, each useful as a vitamin B6 dependent enzyme inhibitor, antibacterial agent or antimycotic agent. CONSTITUTION:The 2-amino-2-ethylmalonic ester of formula I (R is H, aryl, aralkyl, cycloalkyl, cycloalkenyl, alkyl, or trialkylsilyl; R is H, alkyl or aralkyl; R is H or amino-protecting group), e.g. ethyl-2-acetamido-2-ethoxycarbonyl-4- phenyl-3-butynoic ester; the second objective ynamide derivative of formula II, e.g. ethyl 2-N-phenylethylacetamidoacetate; and the third objective 3- alkylthio-2-amico-3-butenic acid derivative, e.g. ethyl-2-acetamido-(E)-ethylthio-4- phenyl-3-butenoic ester. The respective compounds of the formulas I, II, and III, can be obtained according to the respective reaction formulas.