Title:
保護されたアミジンの製造方法
Document Type and Number:
Japanese Patent JP2008531535
Kind Code:
A
Abstract:
A process for preparing a protected amidine group of formula (I): wherein R6 represents, for example, C1-10 alkyl (optionally substituted), aryl, C1-3 alkylaryl or C1-3 alkyloxyaryl; which comprises reacting a nitrile containing compound with an oxyamine of formula (II): R6ONH2 wherein R6 is as defined above for (I); in the presence of a thio-keto activating agent of formula (III): HS-Ry, -C(O)-Z wherein Z is -(1-4C)alkyl, -OH, -O-(1-4C)alkyl, -SH, -S(1-4C)alkyl, -NH2, -NH(1-4C)alkyl or -N[(1-4C)alkyl]2; Ry is (1-2C)alkyl (optionally substituted); or Z and Ry are linked so as to form a 5- or 6-membered ring of formula (IV): wherein X is -CH2-, -O-, -NH- or -N(1-4C)alkyl; p is 1 or 2; m is 1 or 2 and Rz is independently selected from H, (1-4C)alkyl, halo and amino.
Inventors:
Al-Suffer, Philas
Berlin, Stephan
Musir, Thibor
Shivadasan, Shiva Prasad
Berlin, Stephan
Musir, Thibor
Shivadasan, Shiva Prasad
Application Number:
JP2007556659A
Publication Date:
August 14, 2008
Filing Date:
February 22, 2006
Export Citation:
Assignee:
AstraZeneca Activrag
International Classes:
C07C259/18; C07C259/14; C07D205/04; C07D209/18
Domestic Patent References:
| JP2004506039A | 2004-02-26 | |||
| JP2004520290A | 2004-07-08 | |||
| JP2005504057A | 2005-02-10 | |||
| JP2000517325A | 2000-12-26 |
Attorney, Agent or Firm:
Kazuo Shamoto
Shinjiro Ono
Yasushi Kobayashi
Akio Chiba
Hiroyuki Tomita
Takumi Terachi
Shinjiro Ono
Yasushi Kobayashi
Akio Chiba
Hiroyuki Tomita
Takumi Terachi