Title:
4-AMINO-DELTA4,6-STEROIDS AND ITS USE AS 5ALPHA-REDUCTASE INHIBITOR
Document Type and Number:
Japanese Patent JP3021818
Kind Code:
B2
Abstract:
PURPOSE: To industirially advantageously obtain the compd. of the subject having 5α-reductase inhibiting activity for the treatment for acne and postatomegaly by allowing a 4,5-epoxy compd. of steroid to react with sodium azide in an inert solvent.
CONSTITUTION: A 4,5-epoxy compd. of steroid expressed by formula I is allowed to react with sodium azide at 100°C in an inert solvent in the presence of sulfuric acid to obtain the objective 4-amino-steroid expressed by formula II (R is H, 1 to 4c alkyl). In formula I, R1 is 2 to 6C alkanoyl, (2 to 6C alkyl)-(OZ1)2 (Z1 is H, 1 to 6C alkyl 1 to 6C alkanoyl, benzoyl, etc.); R2 is H or with R1 to form OCH2CH2CH2, etc.; R5 is H, methyl; X is O, H2; Z is H, 1 to 6C alkyl; the dotted line means that double bonds may be optionally added. The epoxy steroid. is, for example, [e.g. N-(1,1-dimethylethyl)-4,5-epoxy-3- oxoandrostance-17β-carboxyamide].
Inventors:
Philip Ma-bin Wate Love
Application Number:
JP21416291A
Publication Date:
March 15, 2000
Filing Date:
August 01, 1991
Export Citation:
Assignee:
Merrell Dow Fa-Mass-Tikal's Parakeet-Polated
International Classes:
A61K8/00; A61K31/56; A61K31/57; A61K8/63; A61K31/575; A61P5/00; A61P13/02; A61P15/00; A61P17/00; A61Q19/00; C07J3/00; C07J7/00; C07J9/00; C07J41/00; C07J71/00; (IPC1-7): C07J41/00; A61K7/00; A61K31/575
Attorney, Agent or Firm:
Katsuro Sasai
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