PURPOSE: To obtain a new epi-epi bacidin derivative having an excellent analgesic activity and extremely low toxicity.
CONSTITUTION: This epi-epi bacidin derivative is a compound of formula I (R is a lower alkyl, a lower alkenyl, an aryl, etc.; R' is H, a lower alkynyl, an acyl, etc., when R' is H, R is not 6-chloro-3-pyridyl) and a salt thereof, e.g. (±)-7 -acetyl-2β-[4-(1 -fluorophenyl)]-7α -azabicyclo[2.2.1]heptane. The above compound is obtained by cyclizing a racemic or an optically active compound of formula II (L is methanesulfonyloxy, p-toluenesulfonyloxy, etc.), preferably in a halogenated hydrocarbon or an aromatic hydrocarbon at the boiling point of the reaction mixture, and alkylating or acylating at need. Further, the compound of the formula II is preferably obtained by using nitromethane and methyl vinyl ketone as starting materials and passing through a new intermediate compound of formula III and an intermediate compound of formula IV successively.
JIYUJIYANNA BAROO
ISHIYUTOBUAAN MORUDOBAI
ESUTERU TEMESHIYUBAARI
CHIYABA SAANTAI JIYUNIA
ATSUTEIRA MAANDEI
GAABORU BURASHIYUKOO
JIYURA SUIMIGU
JIYORUJI RATSUKUSU
SHIYAANDORU DORABANTO
MARUGITSUTO CHIERUGOO
MAARIA SOMOJI
BURANKA RADEI
MAARUTON FUEKETE
KATARIN SEMEREEDEI
ISHIYUTOBUAAN JIERUCHIYAAN
GAABORU GIGURERU
TAMAASHIYU SAARAASHI
