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Title:
GLUTAMIC ACID DERIVATIVE AND ITS PRODUCTION
Document Type and Number:
Japanese Patent JP2698570
Kind Code:
B2
Abstract:

PURPOSE: To obtain a glutamic acid derivative usable as a synthetic intermediate for a sugar-modified polyglutamic acid derivative useful as a drug delivery carrier having organotropic property.
CONSTITUTION: This glutamic acid derivative is expressed by formula I (R3 is 9-fluorenylmethoxycarbonyl; R4 is a carboxyl-protecting group). The compound is produced by reacting the α-amino group of glutamic acid having protected γ-carboxyl group with a reactive derivative of 9-fluorenylmethoxycarboxylic acid, e.g. by reacting the acid with succinimide, protecting the α-carboxyl group and eliminating the protective group of the γ-carboxyl group. The compound of formula I can be converted to a compound of formula II (R2 is glucosyl; (n) is 7-10) by selecting the 9-fluorenylmethoxycarbonyl for the protection of the amino group of glutamic acid. Further, the compound of formula II is converted to a sugar-modified polyglutamic acid derivative of formula III (R1 is OR' or NHR"; R' is H, an alkali metal, etc.; R" is H or a physiologically active substance; the molar ratio of (m) to (k) is 1-100).


Inventors:
Tamio Sugawara
Hiroyuki Iwasawa
Kunihiko Irie
Hideo Nogusa
Hiroshi Susaki
Gonsei Akitoku
Application Number:
JP1996000182579
Publication Date:
January 19, 1998
Filing Date:
July 12, 1996
Export Citation:
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Assignee:
DDS Research Institute Co., Ltd.
International Classes:
A61K47/18; B01J23/44; C07B61/00; C07C269/04; C07C271/18; C07C271/22; (IPC1-7): C07C271/22; C07C269/04
Domestic Patent References:
JP2500749A
Foreign References:
Other References:
SYNTHESIS,1990,(7),571−572
Attorney, Agent or Firm:
Hajime Tsukuni (1 person outside)