Title:
7-クロロ-4-(ピペラジン-1-イル)-キノリンの新規合成方法
Document Type and Number:
Japanese Patent JP2014516065
Kind Code:
A
Abstract:
The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
Inventors:
Walter Kaburi
Roberto Castagnani
Sylvia Almarori
Janandrea Quattrociocchi
Vincentzo Corranjury
Roberto Castagnani
Sylvia Almarori
Janandrea Quattrociocchi
Vincentzo Corranjury
Application Number:
JP2014514030A
Publication Date:
July 07, 2014
Filing Date:
June 05, 2012
Export Citation:
Assignee:
SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE SOCIETA PER AZIONI
International Classes:
C07D215/46
Domestic Patent References:
| JP2005537247A | 2005-12-08 |
Foreign References:
| US20060270852A1 | 2006-11-30 | |||
| WO2009050734A2 | 2009-04-23 | |||
| US3331843A | 1967-07-18 | |||
| CN101440063A | 2009-05-27 |
Other References:
IN 2005MU00639 A, JPN7016001145, 9 December 2005 (2005-12-09), ISSN: 0003314919
ANDREWS, SIMEON; BURGESS, STEVEN J.; SKAALRUD, DEBORAH; KELLY, JANE XU; ET AL: "Reversal Agent and Linker Variants of Reversed Chloroquines: Activities against Plasmodium falcipar", JOURNAL OF MEDICINAL CHEMISTRY, vol. 53(2), JPN6016017376, 2010, pages 916 - 919, ISSN: 0003314923
SINGH T: "ANTIMALARIALS 7-CHLORO-4-(SUBSTITUTED AMINO) QUINOLINES", JOURNAL OF MEDICINAL CHEMISTRY, vol. V14 N4, JPN5014007468, 1 January 1971 (1971-01-01), US, pages 283 - 286, ISSN: 0003314920
SUNDURU, NARESH; SHARMA, MONI; SRIVASTAVA, KUMKUM; RAJAKUMAR, S.; PURI, S. K.; ET AL: "Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with pot", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 17(17), JPN6016017369, 2009, pages 6451 - 6462, ISSN: 0003314921
KUMAR, ASHOK; SRIVASTAVA, KUMKUM; RAJA KUMAR, S.; PURI, S. K.; CHAUHAN, PREM M. S.: "Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20(23), JPN6016017373, 2010, pages 7059 - 7063, ISSN: 0003314922
新実験化学講座１ 基本操作Ｉ, JPN6016045927, 20 March 1978 (1978-03-20), pages 318 - 325, ISSN: 0003452654
ANDREWS, SIMEON; BURGESS, STEVEN J.; SKAALRUD, DEBORAH; KELLY, JANE XU; ET AL: "Reversal Agent and Linker Variants of Reversed Chloroquines: Activities against Plasmodium falcipar", JOURNAL OF MEDICINAL CHEMISTRY, vol. 53(2), JPN6016017376, 2010, pages 916 - 919, ISSN: 0003314923
SINGH T: "ANTIMALARIALS 7-CHLORO-4-(SUBSTITUTED AMINO) QUINOLINES", JOURNAL OF MEDICINAL CHEMISTRY, vol. V14 N4, JPN5014007468, 1 January 1971 (1971-01-01), US, pages 283 - 286, ISSN: 0003314920
SUNDURU, NARESH; SHARMA, MONI; SRIVASTAVA, KUMKUM; RAJAKUMAR, S.; PURI, S. K.; ET AL: "Synthesis of oxalamide and triazine derivatives as a novel class of hybrid 4-aminoquinoline with pot", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 17(17), JPN6016017369, 2009, pages 6451 - 6462, ISSN: 0003314921
KUMAR, ASHOK; SRIVASTAVA, KUMKUM; RAJA KUMAR, S.; PURI, S. K.; CHAUHAN, PREM M. S.: "Synthesis of new 4-aminoquinolines and quinoline-acridine hybrids as antimalarial agents", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20(23), JPN6016017373, 2010, pages 7059 - 7063, ISSN: 0003314922
新実験化学講座１ 基本操作Ｉ, JPN6016045927, 20 March 1978 (1978-03-20), pages 318 - 325, ISSN: 0003452654
Attorney, Agent or Firm:
Takuji Yamada
Aoyama Aoi
Michiko Matsutani
Mitsutaka Iwasaki
Aoyama Aoi
Michiko Matsutani
Mitsutaka Iwasaki