Title:
4,1-BENZOXAZEPINE DERIVATIVE AND ITS USE
Document Type and Number:
Japanese Patent JP3283628
Kind Code:
B2
Abstract:
PURPOSE: To obtain a new compound having action to inhibit a squalene synthetic enzyme and antifungal action and useful in treatment for hypercholesterolemia, coronary arteriosclerotic disease, infection of fungi, etc.
CONSTITUTION: A compound of formula I (R1 is H or hydrocarbon; R2 and R3 are H, lower alkyl, phenyl or aromatic heterocycle; X is direct bond or spacer ; Y is carboxyl, OH, amino, phenyl, etc.; the ring A is substitutive), e.g. trans-1-isobutyl-2-oxo-5-(O-tolyl)-l,2,3,5-tetrahydro-4,1-benzoxazepine-3- aceticacid. The compound of formula I is obtained by using a compound of formula II as a starting substance, passing through 4 steps, introducing into a compound of formula III (R4 is 1-8C alkyl or aralkyl) and treating the compound of formula III with a metal hydride complex compound (e.g. lithium aluminum hydride) in a solvent (e.g. methanol) at -20 to 100°C.
Inventors:
Hidefumi Yukimasa
Ryuichi Usazawa
County Jeongseong
Kazuaki Kitano
Ryuichi Usazawa
County Jeongseong
Kazuaki Kitano
Application Number:
JP11785793A
Publication Date:
May 20, 2002
Filing Date:
April 20, 1993
Export Citation:
Assignee:
Takeda GmbH
International Classes:
A61K31/55; A61K31/553; A61P3/06; A61P31/04; A61P31/10; A61P43/00; C07D267/14; C07D413/06; (IPC1-7): C07D267/14; A61K31/553; A61P3/06; A61P43/00
Attorney, Agent or Firm:
Shintaro Nogawa
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