| 摘要 |
<p>1425429 Benzoxazolinone derivatives INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE 24 June 1974 [26 June 1973] 27952/74 Heading C2C Novel compounds have the Formula I: m which R 1 represents a hydrogen atom, an unsubstituted or substituted alkyl group containing 1 to 6 carbon atoms, an unsubstituted or substituted phenyl or benzyl group or a thienyl group, R 2 represents a hydrogen atom or an alkyl group containing 1 to 6 carbon atoms, and X represents a hydrogen atom and Y represents a hydroxy group or X and Y together represent an oxo group. The compounds of Formula I in which R 1 is other than a hydrogen atom are obtained by reacting in the presence of polyphosphoric acid a compound of Formula II: with an acid of formula R 1 COOH or a functional derivative thereof (e.g. anhydride or chloride) to form a compound of Formula I wherein X and Y together represent an oxo-group, the corresponding alcohol of Formula I being obtained therefrom by reduction (e.g. NaBH 4 ). The compounds of Formula I wherein R 1 represents a hydrogen atom are prepared by reacting in the presence of polyphosphoric acid a compound of Formula II with hexamethylenetetramine to form the 6-formyl benzoxazolinone derivative of Formula I, the corresponding hydroxymethyl derivative being again obtained by reduction. The examples prepare compounds of Formula I in which R 1 is -CH 3 , -C 2 H 5 , -CH 2 Cl, -C 6 H 5 , -CH 2 C 6 H 5 , thienyl and hydrogen and R 2 is hydrogen or -CH 3 .</p> |
