| abstract |
PURPOSE: To obtain the subject compounds useful as a fungicide, etc., in a mild reaction condition in a high yield and at a low cost without using a special apparatus by reacting a new substituted allylamine derivative with a substituted acetylene derivative in the presence of Pd catalyst. n CONSTITUTION: A compound of formula I (W is halogen; Z is eliminative group) is reacted with an amine of formula II [R 11 is H, alkyl, haloalkyl, alkenyl, etc.; R 21 is H, formula III (R 3 is H or alkyl; R 4 is H, OH, alkyl, etc.), etc.] to obtain a new substituted allylamine of formula IV. The resultant new compound is reacted with an acetylene derivative of formula V (R 7 is H, alkyl, phenyl, etc.) in the presence of Pd catalyst to obtain a compound of formula VI. N-alkylation is further carried out as necessary, thus obtaining the objective eneyne derivative of formula VII (R 1 is H, alkyl, alkenyl, etc.; R 2 is formula III, etc.). The resultant compound is useful as a fungicide, a compound capable of selective inhibition of squalene epoxydase and having a remarkable anticholesterol effect and a precursor thereof. n COPYRIGHT: (C)1991,JPO&Japio |