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US 2014/0309437 A1Published application
Process for the preparation of pharmaceutical intermediates
AssigneeDipharma Francis S.R.L.
InventorsMarco ARTICO, Emanuele ATTOLINO
Life of this patent
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Abstract
Process for the preparation of intermediates that are useful in the synthesis of active pharmaceutical ingredients (API), in particular active in the central nervous system.
Claims14
A process for preparing a compound of formula (I):
- wherein X is O or S, comprising cyclizing a compound of formula (II):
- wherein X is as defined above, in the presence of a catalytic amount of FeCl3 which is between about 0.05% and 10% molar.
(canceled)
A process for preparing Doxepin, (3E)-3-(6H-benzo[c][1]benzoxepin-11-ylidene)-N,N-dimethylpropan-1-amine, or Dothiepin, (3Z)-3-(6H-benzo[c][1]benzothiepin-11-ylidene)-N,N-dimethylpropan-1-amine, comprising utilizing, as starting material, a compound of formula (II):
- wherein X is O or S respectively, and cyclizing the compound in the presence of a catalytic amount of FeCl3 which is between about 0.05% and 10% molar in order to obtain a compound of formula (I):
- wherein X is as defined above;
- the compound of formula (I) as prepared by this process is then converted into Doxepin or Dothiepin according to known methods.
Dependencies are inferred from the claim text.