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Title:
PRODUCTION OF PROTECTED HYDROXY GROUP-CONTAINING HETEROCYCLIC COMPOUND
Document Type and Number:
Japanese Patent JP3396066
Kind Code:
B2
Abstract:

PURPOSE: To obtain the subject compound in high yield by reacting a compound having an amino group and a hydroxyl group with a halogenated aralkyl or an acid halide in the presence of an inorganic weak base.
CONSTITUTION: A compound of formula I(X1 is NH, S or O; X2 is CH or N; R1 is an organic group) is made to react with a halogenated aralkyl or an acid halide in the presence of an inorganic weak base (e.g. potassium hydrogen carbonate) in a solvent (e.g. acetone) at 0-50°C to provide the objective compound of formula II (R2 is a residue being removed a halogen atom from the halogenated aralkyl or the acid halide, e.g. an aralkyl or an acyl). A hyterocyclic compound in which only amino group is selectively protected in a state where side reaction is suppressed and hydroxyl group is left as it is obtained by using a specific inorganic weak base. The base is used in an equivalent of 1-3 times based on the compound of formula I. As the halogenated aralkyl, chlorotriphenylmethyl is exemplified and as the acid halide, acetyl chloride is exemplified.


Inventors:
Shinichiro Koyanagi
Shozo Tsuchiya
Application Number:
JP24308293A
Publication Date:
April 14, 2003
Filing Date:
September 29, 1993
Export Citation:
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Assignee:
Tokuyama Corporation
International Classes:
C07D233/88; C07D263/48; C07D271/06; C07D277/20; C07D277/42; C07D277/46; C07D285/08; C07D249/14; (IPC1-7): C07D233/88; C07D249/14; C07D263/48; C07D271/06; C07D277/42; C07D277/46; C07D285/08