Novel Process for the Synthesis of Docosanol
AssigneeBiophore India Pharmaceuticals PVT. Ltd.
InventorsManik Reddy PULLAGURLA, Jagadeesh Babu RANGISETTY
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Abstract
The present invention relates to a novel process for the preparation of Docosanol (I). More particularly, the invention relates to a novel process for the preparation of Docosanol (I) in a substantially pure form with a purity level of greater than 99.5%. The invention also relates to novel crystalline forms of Docosanol (I) and process for preparation thereof.
Claims14
A high purity Docosanol (I), wherein said Docosanol has a purity of greater than 99.5% and one or more of the following;
- (iii) less than 0.15% n-Tetracosanol as impurity A;
- and
- (iv) less than 0.15% Icosanal as impurity B.
A process for the preparation of Docosanol (I), comprising:
- a) oxidation of 1-eicosanol (IV) to form icosanal (III) by treating with a suitable oxidizing agent and base;
- b) Wittig reaction between icosanal (III) and a Wittig reagent to form (E)-ethyl docos-2-enoate (II);
- c) reduction of (E)-ethyl docos-2-enoate (II) using suitable reducing agent to form Docosanol (I);
- and
- d) optionally, purifying Docosanol (I).
A process for the purification of Docosanol (I), comprising:
- 5) combining Docosanol (I) with aprotic solvent or protic solvent or mixtures thereof;
- 6) heating the mixture of step 1) between 50° C. to 65° C.;
- 7) cooling the mixture of step 2) between 0° C. to 35° C.;
- and
- 8) isolating Docosanol (I) by filtering under vacuum.
A crystalline Form A of Docosanol, characterized by X-ray powder diffraction (XRPD) pattern having peaks expressed as 20 values at about 3.51, 5.28, 7.05, 8.82 and 21.63±0.2 degrees.
Dependencies are inferred from the claim text.