Lurasidone key intermediate preparation method

A technology of lurasidone and intermediates, applied in the field of compound synthesis, can solve the problems of low total yield, high cost, and large consumption of resolution reagents, and achieve the effect of easy industrial production and simple operation
CN106946872AInactive Publication Date: 2017-07-14CHANGZHOU VOCATIONAL INST OF ENG
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Patent Information

Authority / Receiving Office
CN Β· China
Patent Type
Applications(China)
Current Assignee / Owner
CHANGZHOU VOCATIONAL INST OF ENG
Publication Date
2017-07-14
Estimated Expiration
Not applicable Β· inactive patent

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Abstract

The present invention relates to a lurasidone key intermediate preparation method, and belongs to the technical field of compound synthesis. According to the method, when 4,-(1,2-benzisothiazol-3-yl)-(3aR,7aR)-octahydrospiro(2H-isoindole-2,1-piperazine)methanesulfonate is generated, 4-(1,2-benzisothiazol-3-yl)-1-piperazine is adopted as a raw material, the 4-(1,2-benzisothiazol-3-yl)-1-piperazine, (1R,2R)-1,2-bis(methanesulfonyloxymethyl)cyclohexane and potassium carbonate are subjected to a reaction in a solvent toluene, and a cyclodextrin phase transfer catalyst is added to the reaction system. According to the present invention, by using the cyclodextrin as the phase transfer catalyst, the incomplete reaction problem is solved, and the yield is substantially improved.
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Description

technical field

[0001] The invention relates to a method for preparing a key intermediate of lurasidone, belonging to the technical field of compound synthesis. Background technique

[0002] Lurasidone hydrochloride (Lurasidone HCl, 1) chemical name: (3aR,4S,7R,7aS)-2-[(1R,2R)-2-[4-(1,2-benzisothiazole-3- Base) piperazin-1-ylmethyl] cyclohexylmethyl] hexahydro-1H-4,7-methylisoindole-1,3-dione hydrochloride, which is developed by Japan Dainippon Sumitomo Atypical antipsychotic drugs, approved by the US FDA on October 28, 2010, for the first-line treatment of patients with schizophrenia, and its trade name is Latuda. In July 2013, it was approved for the treatment of bipolar depression in adults. Lurasidone (2) is the key intermediate of lurasidone hydrochloride.

[0003] There are not many synthetic methods of lurasidone (2) reported in the literature, and the practical ones are mainly divided into five kinds.

[0004] Method 1, U.S. Patent (US 5532372A, 1996-07-02) uses ...

Claims

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