Title:
POLYMORPHIC FORM OF 4-[3-(4-CYCLOPROPANECARBONYL-PIPERAZINE-1-CARBONYL)-4-FLUORO-BENZYL]-2H-PHTHALAZIN-1-ONE
Document Type and Number:
Japanese Patent JP2013136607
Kind Code:
A
Abstract:
To provide improved methods of synthesis of a particular phthalazinone derivative.
This invention relates to: methods of synthesis of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one from 4-[4-fluoro-3-(piperazine-1-carbonyl)-benzyl]-2H-phthalazin-1-one; and a method of reacting 2-fluoro-5-(4-oxo-3,4-dihydro-phthalazin-1-ylmethyl)-benzoic acid with 1-(cyclopropylcarbonyl)piperazine or a mineral acid salt thereof in the presence of an amide coupling agent from 2-fluoro-5-(4-oxo-3,4-dihydro-phthalazin-1-ylmethyl)-benzoic acid.
Inventors:
MENEAR KEITH ALLAN
OTTRIDGE ANTHONY PETER
LONDESBROUGH DEREK JOHN
HALLETT MICHAEL RAYMOND
MULLHOLLAND KEITH RAYMOND
PITTAM JOHN DAVID
LAFFAN DAVID DERMOT PATRICK
ASHWORTH IAN WOODWARD
JONES MARTIN FRANCIS
CHERRYMAN JANETTE HELEN
OTTRIDGE ANTHONY PETER
LONDESBROUGH DEREK JOHN
HALLETT MICHAEL RAYMOND
MULLHOLLAND KEITH RAYMOND
PITTAM JOHN DAVID
LAFFAN DAVID DERMOT PATRICK
ASHWORTH IAN WOODWARD
JONES MARTIN FRANCIS
CHERRYMAN JANETTE HELEN
Application Number:
JP2013025205A
Publication Date:
July 11, 2013
Filing Date:
February 13, 2013
Export Citation:
Assignee:
KUDOS PHARM LTD
International Classes:
C07D237/32; A61K31/502; A61P7/04; A61P9/00; A61P9/10; A61P25/00; A61P31/12; A61P35/00; A61P43/00
Domestic Patent References:
| JP2006519827A | 2006-08-31 |
Other References:
JPN6014016243; 日本化学会編 第４版実験化学講座２２，有機合成ＩＶ 酸・アミノ酸・ペプチド , 19921130, 第１４４〜１４５頁, 丸善株式会社
Attorney, Agent or Firm:
Yusuke Hiraki
Ishii Teiji
Satoshi Fujita
Eiichi Arai
Ishii Teiji
Satoshi Fujita
Eiichi Arai
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