A novel preparative method of psilocin was established in only five steps from indole-3-carbaldehyde in 50% overall yield.psilocin2 ( 1 , Scheme 1) and psilocybin2 (2) are known to enter the central nervoussystem through the gastrointestinal trac? and cause powerful psychotomimetic effect.2-4~1thoughconsiderable efforts2.4have been devoted to the syntheses of psilocin analogs, there still remains to establish structure-activity relationships.While, recently, psychotic diseases such as depression, schizophrenia.Alzheimer's disease, and so on, are becoming social problems and the development for their medicines has been waited.With a hope to find a lead compound among psilocin analogs possesing suitable pharmacological effects, we have needed an effective preparative method of 1 which makes it possible to pursue systematic structure-activity relationship studies.In this paper, we wish to report the desired five-step preparative method of 1 from indole-3-carbaldehyde (3) as shown in Scheme 1.We have already reported one pot procedur& for preparing 4a from indole-3-carbaldehyde (3).The overall yield of
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Somei et al. (1998) studied this question.