# US 10,118,899 B2 · Production method of enzalutamide crystal form

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- Number: US 10,118,899 B2
- Document ID: US10118899B2
- Status: Granted
- Kind: B2
- Application number: 15/577,007
- Filed: 2016-05-27
- Published: 2018-05-31
- Granted: 2018-11-06
- Earliest claimed: 2015-05-29
- Assignees: Astellas Pharma Inc.
- Applicants: Astellas Pharma Inc.
- Inventors: Yusuke Suzuki; Shuichi Nakagawa; Tsuyoshi Kitamura
- Web page: https://patentgrep.com/patent/US10118899B2

## CPC

- C07D 233/86: Oxygen and sulfur atoms, e.g. thiohydantoin
- A61P 35/00: Antineoplastic agents
- C07C 331/28: having isothiocyanate groups bound to carbon atoms of six-membered aromatic rings
- C30B 7/00: Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions (from molten solvents C30B9/00; by normal or gradient freezing C30B11/00; under a protective fluid C30B27/00)
- C30B 33/00: After-treatment of single crystals or homogeneous polycrystalline material with defined structure (C30B31/00 takes precedence)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C30B: SINGLE-CRYSTAL GROWTH (by using ultra-high pressure, e.g. for the formation of diamonds, B01J3/06); UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL (zone-refining of metals or alloys C22B); PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE (casting of metals, casting of other substances by the same processes or devices B22D; working of plastics B29; modifying the physical structure of metals or alloys C21D, C22F); SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE (for producing semiconductor devices or parts thereof H10); APPARATUS THEREFOR

## Abstract

The present invention aims to provided a novel production method of an enzalutamide crystal form in which wet crystals of enzalutamide are obtained in a step of crystallizing in the production process of the enzalutamide crystal form, and then 2-propanol which is solvated with enzalutamide and the B-type crystals are reduced. The present invention relates to a production method of an enzalutamide crystal form, which comprises a step of crystallizing for obtaining wet crystals of enzalutamide, and a step of drying the wet crystals, and comprises a step of washing using a mixed solvent of a good solvent and a poor solvent after the step of crystallizing.

## Claims

### Claim 1

A method of producing a crystal form of enzalutamide:
comprising a step of crysallizing for obtaining wet crystals of enzalutamide and a step of drying the wet crystals, wherein the method comprises a step of washing using a mixed solvent of a good solvent and a poor solvent after the step of crystallizing, wherein the good solvent is isopropyl acetate and the poor solvent is n-heptane.