摘要 |
A Pictet-spengler reaction process for preparing tetrahydroisoquinolines of the formula 1 where R1 and R2 are each independently C1-3 alkyl or R1 and R2 together form C2-7 alkylene N is 0-2 R3 is hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, -CF3, -OCF3 and -OH Ts is para-toluensulfonyl By reacting a compound II with a suitable Lewis acid like boron trifluoretherate(BF3.OEt2), aluminum chloride, zinc chloride, magnesium bromide, ferric chloride (FeCl3) in formaldehyde generating solvent. |