Process for synthesizing anhydroecgonine derivative

C - Chemistry – Metallurgy – 07 – D

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C07D 451/02 (2006.01) C07K 5/083 (2006.01)

Patent

CA 2331029

The present invention relates to a process for synthesizing an anhydroecgonine derivative without using cocaine as a starting material, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative as an intermediate for the synthesis. The present invention provides a process for synthesizing an anhydroecgonine derivative which comprises reacting a cycloheptatriene derivative represented by the formula (1): (see formula 1) with a primary amine, a salt thereof or ammonia in the presence of a base to obtain an anhydroecgonine derivative, and a process for synthesizing a phenyl- tropane derivative by using said anhydroecgonine derivative. In the formula (1), n is an integer of 0 or 1; and R1 is a cyano group in the case of n being 0, and R1 is selected from an alkyl group and an aralkyl group in the case of n being 1.

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