Title:
PRODUCTION OF ALPHA 1L-ADRENORECEPTORS ANTAGONIST
Document Type and Number:
Japanese Patent JP3276342
Kind Code:
B2
Abstract:
PROBLEM TO BE SOLVED: To economically obtain the subject compound useful as an α11- adrenoreceptor antagonist useful for treating benign prostatic proliferation.
SOLUTION: This compound of formula I [wherein, R is H, methyl of fluoro; L is a leaving group] [e.g. 3-(3-chloropropyl)-tosylthymine] is produced by reacting a compound of formula II with a compound of formula III under a basic condition, by reacting the product with a compound of formula IV under a basic condition to obtain a compound of formula V, following by the cleavage of a tosyl group of the compound of formula V in the presence of a cleavage agent (e.g. sodium methoxide). It is preferable that the above reaction is conducted in the presence of such a base as Et3N, K2CO3, NaOH in such a solvent as CH3CN/H2O and H2O at a temp. of about 15-25°C.
Inventors:
Robert Clark Chapman
Joren Perkins
Joren Perkins
Application Number:
JP8508899A
Publication Date:
April 22, 2002
Filing Date:
March 29, 1999
Export Citation:
Assignee:
F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT
International Classes:
A61K31/00; A61K31/505; A61K31/513; A61P13/00; A61P13/08; A61P43/00; C07D239/54; C07D239/553; (IPC1-7): C07D239/54
Domestic Patent References:
| JP9100269A |
Attorney, Agent or Firm:
Hajime Tsukuni (1 person outside)
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