PRODUCTION OF TERAZOSIN HYDROCHLORIDE DIHYDRATE AND INTERMEDIATE

Title:

PRODUCTION OF TERAZOSIN HYDROCHLORIDE DIHYDRATE AND INTERMEDIATE

Document Type and Number:

Japanese Patent JP2711230

Kind Code:

B2

Abstract:

PURPOSE: To provide a method for efficiently producing 1-(4-amino-6,7- dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine (terazosin) hydrochloride dihydrate in high yield and obtain an intermediate compound of the method called as anhydrous crystal modification seed of IV type of terazosin.
CONSTITUTION: This method for producing 1-(4-amino)-6,7-dimethoxy-2- quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate includes (a) a stage reacting 4-Amino-2 chloro-6,7-dimethoxy-quinazoline with N-(2- tetrahydrofuroyl)piperazine in an anhydrous polar organic solvent in the absence of an acid scavenger to produce IV-form crystalline variable seed of anhydrous 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)4-(2-tetrahydrofuroyl)piperazine hydrochloride and (b) a stage converting a product of the stage (a) to 1-(4-amino-6,7- dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate.

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Inventors:

Anthony Manino
Roger F Henry
Wayne Earl Hateman
Bruce Davryu Holom

Application Number:

JP5743595A

Publication Date:

February 10, 1998

Filing Date:

March 16, 1995

Export Citation:

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Assignee:

ABBOTT LABORATORIES

International Classes:

A61K31/505; A61P9/00; A61P9/12; C07D405/12; (IPC1-7): C07D405/12

Domestic Patent References:

JP578352A

Attorney, Agent or Firm:

Yoshio Kawaguchi (2 outside)

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