PURPOSE: To provide a novel boron compd. useful as an intermediate for synthesizing a quinoline deriv., pyridine deriv. and imidazole deriv. having the activity to suppress angiotensin II.
CONSTITUTION: The compd. of formula I {Q is formula II, III [R1 is H, phenyl, etc.; R2 is H, cyano, etc.; R3, R4 are H, amino, etc.; R4 is H, halogeno, etc.; T1 is H, 1 to 8C alkyl, etc.; T2 is H, nitro, etc.; T3 is halogeno, amino, etc.; T4 is A1, A2, E (A1 is carbonyloxy; A2 is 1 to 6C alkylene, E is OH, etc.), etc.; Y1 is H, 1 to 4C alkoxy, etc.; G1, G2 are OH, 1 to 6C alkyl, etc.} or its salt; for example, 4-[(2-ethyl-5,6,7,8-tetrahydroquinoline-4-yl)oxymethyl]phenylboric acid. The compd. is obtd. by alkylating the compd. of formula IV (R1 is exclusive of H) by the compd. of formula V (Hal is a dissociation group). The reaction is generally executed at 10 to 100°C in a polar solvent in the presence of a base, such as sodium methoxide.
SUTANREI AANORUDO RII
DEEBITSUDO MAIKERU GURANBUIRU
RIN PAUERU
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