# US 7,608,711 B2 · Process for the preparation of ziprasidone

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- Number: US 7,608,711 B2
- Document ID: US7608711B2
- Status: Granted
- Kind: B2
- Application number: 11/595,861
- Filed: 2006-11-13
- Published: 2007-05-24
- Granted: 2009-10-27
- Earliest claimed: 2005-11-18
- Assignees: Dipharma Francis S.R.L.
- Inventors: Jacopo Zanon; Oscar Martini; Francesco Ciardella; Luca Gregori; Federico Sbrogio; Andrea Castellin
- Web page: https://patentgrep.com/patent/US7608711B2

## CPC

- C07D 417/12: linked by a chain containing hetero atoms as chain links
- C07D 209/34: in position 2
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.

## Claims

### Claim 1

A process for the preparation of ziprasidone (I) or a pharmaceutically acceptable salt thereof,
which comprises
a) reducing a compound (III)
by treatment with an alkali metal borohydride to yield a compound (V)
b) reducing compound (V) to yield a compound (II)
c) reacting compound (II) with a compound (IV)
d) and, if desired, converting compound (I) to a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

The process as claimed in claim 1, wherein the reduction of a compound (III) is carried out in a solvent selected from water, a C1-C4 alkanol, aliphatic cyclic or alicyclic ethers, glycols, and acetic acid.

### Claim 3 (depends on 1)

The process as claimed in claim 1, wherein a compound (III) is reduced by treatment with sodium borohydride in ethanol.

### Claim 4 (depends on 1)

The process as claimed in claim 1, wherein the reaction between a compound (II) and a compound (IV) is carried out in homogeneous phase.

### Claim 5 (depends on 4)

The process as claimed in claim 4, wherein the reaction is carried out in dimethylsulfoxide, at a temperature approx. ranging from 90 to 110° C.