Title:
PROCESS FOR PRODUCTION OF PHENYLALANINE DERIVATIVES HAVING QUINAZOLINEDIONE SKELETONS AND INTERMEDIATES FOR THE PRODUCTION
Document Type and Number:
WIPO Patent Application WO/2008/062859
Kind Code:
A1
Abstract:
A process for the production of phenylalanine derivatives having quinazolinedione
rings as represented by the general formula (1) or pharmaceutically acceptable
salts thereof:(1) which comprises the following steps (a), (b) and (c): the
step (a) of reacting an acylphenylalanine derivative represented by the general
formula (2): (2) with a carbonyl-introducing agent and a specific
anthranilic acid derivative to form a corresponding carboxy asymmetric urea
derivative, the step (b) of converting the carboxy asymmetric urea derivative
into a corresponding quinazolinedione in the presence of a carboxyl-activating
agent, and the optional step (c) comprising the N-alkylation step of replacing
the hydrogen atom attached to the nitrogen atom constituting the quinazoline-
dione ring by an alkyl group with an N-alkylating agent and/or the deblocking
step of deblocking R3' (a group corresponding to R3) when R3' is in
a protected state. According to the process, phenylalanine derivatives having
quinazolinedione skeletons can be produced in high yield favorable for industrialization.
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Inventors:
KATAOKA NORIYASU (JP)
OKADO KOTARO (JP)
YAMADA TATSUHIRO (JP)
FUJITA KOICHI (JP)
SUZUKI TAMOTSU (JP)
OKUZUMI TATSUYA (JP)
SUGIKI MASAYUKI (JP)
TATARA AKINORI (JP)
OKADO KOTARO (JP)
YAMADA TATSUHIRO (JP)
FUJITA KOICHI (JP)
SUZUKI TAMOTSU (JP)
OKUZUMI TATSUYA (JP)
SUGIKI MASAYUKI (JP)
TATARA AKINORI (JP)
Application Number:
PCT/JP2007/072615
Publication Date:
May 29, 2008
Filing Date:
November 22, 2007
Export Citation:
Assignee:
AJINOMOTO KK (JP)
KATAOKA NORIYASU (JP)
OKADO KOTARO (JP)
YAMADA TATSUHIRO (JP)
FUJITA KOICHI (JP)
SUZUKI TAMOTSU (JP)
OKUZUMI TATSUYA (JP)
SUGIKI MASAYUKI (JP)
TATARA AKINORI (JP)
KATAOKA NORIYASU (JP)
OKADO KOTARO (JP)
YAMADA TATSUHIRO (JP)
FUJITA KOICHI (JP)
SUZUKI TAMOTSU (JP)
OKUZUMI TATSUYA (JP)
SUGIKI MASAYUKI (JP)
TATARA AKINORI (JP)
International Classes:
C07C233/51; C07D239/96; C07C237/40; C07C265/12; C07C271/22; C07C271/28; C07C275/42
Domestic Patent References:
| WO2007141473A1 | 2007-12-13 | |||
| WO2007038571A2 | 2007-04-05 | |||
| WO2005009969A1 | 2005-02-03 | |||
| WO2001068586A2 | 2001-09-20 | |||
| WO2004074264A1 | 2004-09-02 | |||
| WO2002016329A1 | 2002-02-28 | |||
| WO2005061466A1 | 2005-07-07 | |||
| WO2002016329A1 | 2002-02-28 | |||
| WO2004074264A1 | 2004-09-02 | |||
| WO2005061466A1 | 2005-07-07 |
Foreign References:
| JPS6230770A | 1987-02-09 | |||
| JPS5246040A | 1977-04-12 | |||
| JPH11505849A | 1999-05-25 |
Other References:
T.W. GREEN; P.G.M. WOOTZ: "Protective Groups in Organic Synthesis", 1999, JHON WILEY & SONS, INC.
"Organic Syntheses Collective", 1973, WILEY, pages: 201 - 204
HETEROCYCLE, vol. 51, no. 7, 1999, pages 1543 - 1561
"Organic Syntheses Collective", 1973, WILEY, pages: 201 - 204
HETEROCYCLE, vol. 51, no. 7, 1999, pages 1543 - 1561
Attorney, Agent or Firm:
KUMAKURA, Yoshio et al. (Shin-Tokyo Bldg.3-1, Marunouchi 3-chom, Chiyoda-ku Tokyo 55, JP)
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