Title:
GRISEOLIC ACID MONOESTER DERIVATIVE
Document Type and Number:
Japanese Patent JP07316183
Kind Code:
A
Abstract:
PURPOSE: To obtain a new compound having excellent intraocular pressure- lowering action and useful as an excellent therapeutic agent for glaucoma.
CONSTITUTION: A compound of formula I (R1 and R2 are each H, OH, etc.; R3 and R4 are each H or R3 and R4 together exhibit a single bond; either one of R5 and R6 is H and the other is a protecting group removed in eyes) and its salt, e.g. griseolic acid-9'-pivaloyloxymethylester. The compound is obtained by reacting, e.g. a raw material compound of formula II with an one equivalent esterifying reagent of the formula R5' -X or R6' -X (X is a halogen, acetoxy, etc.) at a room temperature in a solvent such as DMF in the presence of 1,8- diazabicylo[5.4.0]undec-7-ene which is a deacidifying agent.
Inventors:
Kaneko, Masakatsu
Kimura, Misako
Kamogari, Makoto
Yokoyama, Tomihisa
Yamazaki, Mitsuo
Kimura, Misako
Kamogari, Makoto
Yokoyama, Tomihisa
Yamazaki, Mitsuo
Application Number:
JP1994000321851
Publication Date:
December 05, 1995
Filing Date:
December 26, 1994
Export Citation:
Assignee:
SANKYO CO LTD
International Classes:
C07H19/16; A61K31/52; A61K31/70; A61K31/7042; A61K31/7052; A61K31/7076; A61P27/02; A61P27/06; C07D519/00; (IPC1-7): C07H19/16; A61K31/70
Previous Patent: NUCLEOTIDE COMPOUND AND ITS PRODUCTION
Next Patent: INTERMEDIATE FOR PRODUCING NOVEL 10-SUBSTITUTED STEROID
Next Patent: INTERMEDIATE FOR PRODUCING NOVEL 10-SUBSTITUTED STEROID
