| 摘要 |
PURPOSE:The reduction of a nitrophthalide-isoquinoline with NaBH2S3 or LiBH4 enables industrially advantageous production of the title compound which is used as a medicine without use of a metallic catalyst. CONSTITUTION:A nitro compound of formula III, resulting from condensation reaction between a tetrahydroisoquinolien of formula I (R<1>, R<2> are H, lower alkoxy; R<7> is lower alkyl) and a nitrophthalide of formula II (at least one of R<3>'-R<6>' are nitro), is reduced with NaBH2S3 or LiBH4, preferably in an amount of 1.5-2mol to give the objective compound of formula IV (at least one of R<3>-R<6> is amino). The reduction reaction is carried out in a solvent of 3-20 times the weight of the reactant at 20-60 deg.C for 0.5-30hr. The resultant amino compound is epimerized, when needed, to increase the content of isomer A.
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