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US 12,077,559 B2Granted
Process for the preparation of 3α-hydroxy-5α-pregnan-20-one (brexanolone)
AssigneeIndustriale Chimica S.R.L.
InventorsClaudio Delfrate, Davide Rigamonti, Tea Borelli, Roberto Lenna
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Abstract
The present invention relates to a new process for the synthesis of 3α-hydroxy-5α-pregnan-20-one, commonly known as brexanolone, wherein the corresponding cyclic 20-ketal or cyclic 20-thioketal compound of formula (IV) is deprotected with the use or iodine in an organic solvent: (I).
Claims11
A method for the preparation of 3α-hydroxy-5α-pregnan-20-one (brexanolone) which consists in the deprotection of a cyclic ketal or a cyclic thioketal thereof of general formula (IV) with the use of iodine in an organic solvent, according to the reaction scheme:
- wherein is X═O (oxygen) in the case of ketal and X═S (sulfur) in the case of thioketal, and R is a radical selected among ethylene (—CH2—CH2—), propylene (—CH2—CH2—CH2—) and 2,2-dimethylpropylene (—CH2—C(CH3)2—CH2—).
Dependencies are inferred from the claim text.