PURPOSE: To obtain an isoquinoline deriv. useful as an antitumor or antileukemia drug industrially advantageously by converting a 2-alkoxypyridine deriv. into a metallized deriv. and condensing the resultant product with a heterocyclic compd.
CONSTITUTION: A compd. represented by formula I [wherein R is 1-4C alkyl; and Y is a 4,4-dimethyl-2-oxazolinyl group or a group represented by formula II (wherein R6 and R7 are each R)] is converted into a metallized deriv. represented by formula III [wherein Z1 is Li, MgHal, NnHal, or CeHal (wherein Hal is halogen)] and is then condensed with a compd. represented by formula IV [wherein X is N or C-OR2 (wherein R2 is 1-4C alkyl or benzyl); P is an unstable protective group; and R8 is a group represented by formula V (wherein R1 is H or 1-4C alkyl) or formula VI] to give a compd. represented by formula VII [wherein R1' is R1; and Am is an amino group unsubstituted or substd. by a group represented by formula VIII (wherein R3 to R5 are each H or 1-6C alkyl; and (n) is 1-10)].
ANDORE BUSUKE
JIYANNROBEERU DORUMOWA
ARAN AIMU
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