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Title:
NEW AMINO STEROID COMPOUND
Document Type and Number:
Japanese Patent JPH0559096
Kind Code:
A
Abstract:

PURPOSE: To obtain a new amino steroid compd. having high antiarrhythmic activity and local anesthetic activity and producing no significant effect on cardiac blood output and blood pressure as an aminoalkyl steroid compd. having a specified structure.

CONSTITUTION: 10-Hydroxymethyl steroid of formula I (where R1 and R2 are H, OH or benzyloxy; R3, and R4 are H, alkyl, etc.; and R6 and R7 are H or alkyl) is oxidized with an oxidizing agent such as chromium trioxide. The resultant 10-aldehyde is allowed to react with tosylmethyl isocyanicie and the resultant 10-cyanomethyl body is reduced with lithium aluminum hydride, etc., to form a deriv. of formula II having a 2-aminoethyl group at the 10-position. After this amino group is acylated, the deriv. is converted into a cyclic compd. by reaction in an acidic medium such as concd. hydrochloric acid and the acyl group is reduced and alkylated to obtain the objective amino steroid compd. of formula III [where T is (CH2)n ((n) is 1-2; R5 is H, OH, etc.; and R14 is H, an alkyl, etc.].


Inventors:
REONAADO NOOMAN NAISUTETSUDO
Application Number:
JP969192A
Publication Date:
March 09, 1993
Filing Date:
January 23, 1992
Export Citation:
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Assignee:
SEARLE & CO
International Classes:
A61K31/565; A61K31/57; A61K31/575; A61K31/58; A61K31/585; A61P9/06; A61P23/02; A61P25/02; C07J1/00; C07J21/00; C07J33/00; C07J41/00; C07J51/00; C07J71/00; (IPC1-7): A61K31/565; A61K31/57; A61K31/575; A61K31/58; A61K31/585; C07J41/00
Attorney, Agent or Firm:
Akira Asamura (2 outside)