Starting Materials for the Synthesis of rac-PZQ


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For an inexpensive route to rac-PZQ (and potentially the enantioenriched material), the relevant starting materials (below) are required. While prices may be obtained for these from commercial catalogues, we require realistic prices of these materials on a large (ton) scale to assess whether this approach to PZQ is economically viable. The starting materials are:

Reissert route chemicals:


Cyclohexanoyl chloride
   Cyclohexanoyl chloride
Cyclohexanecarboxylic acid   Cyclohexane carboxylic acid
Example price from Sigma-Aldrich = US$59 for 500 g = 12 cents per gram. Bulk?
       Thionyl Chloride
Chloroacetyl chloride
    Chloroacetyl chloride
Cyanide sources:  KCN (InChI=1/CN.K/c1-2;/q-1;+1)
                      or    NaCN (InChI=1/CN.Na/c1-2;/q-1;+1)

Pictet-Spengler route chemicals:

US$ 96 for 1 L (Sigma-Aldrich)

   (InChI=1/C4H11NO2/c1-6-4(3-5)7-2/h4H,3,5H2,1-2H3 )
US$ 532 for 500 mL (Sigma-Aldrich)