| 摘要 |
<P>PROBLEM TO BE SOLVED: To provide a synthetic method that requires reduced amounts of phosphorus oxychloride, lowered reaction times, reduced temperatures, simplified work-up and isolation, and does not require additional harsh synthetic steps to remove a phenol protecting group. <P>SOLUTION: The present invention is directed to an improved synthetic method for preparing 3,4-dihydroisoquinolines from a phenyl acetic acid derivative and an amine substituted benzene derivative. The present invention is further directed to the preparation of various 3,4-dihydroisoquinolines (Formulae 600 to 602) from the reaction of particular phenyl acetic acid derivatives (Formulae 300 and 301) with phenethylamine derivatives (Formula 400). The reaction product of a phenyl acetic acid derivative and a phenethylamine derivative is an amide compound (Formulae 500 to 502). In the synthetic method, the amide formed can be isolated or the crude product can be further reacted to form a 3,4-dihydroisoquinoline. <P>COPYRIGHT: (C)2013,JPO&INPIT |
