US 7,803,949 B2 · Process for preparation of water-soluble azole prodrugs

Abstract

An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.

Claims24

Dependent claims

A process for preparing a salt represented by Formula (I):

wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group, comprising the steps of:
(a) carrying out a deprotection reaction of a compound represented by Formula (II):
wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group,
(i) in the presence of a first organic acid and a carbocation scavenger or
(ii) in the presence of only a carbocation scavenger to produce a compound represented by Formula (III):
wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group;
and
(b) reacting the compound represented by Formula (III) with lysine in the presence of water, an organic solvent and an acid.

5 more elements

Dependencies are inferred from the claim text.

Facts

Application

12/097,244Filed 20 Dec 2006

Priority

JP 2005-36686220 Dec 2005

Published

US 2009/0192316 A130 Jul 2009

Granted

28 Sep 2010

Term ends

Not estimatedThe source records don’t support an estimate.

Classification5 codes

C07F 9/65583
Containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common…: each of…
A61P 31/10
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics: antimycotics
A61P 43/00
Drugs for specific purposes, not provided for in groups a61p1/00-a61p41/00
C07F
Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen

Process for preparation of water-soluble azole prodrugs

Life of this patent

Process for preparation of water-soluble azole prodrugs

Life of this patent

Abstract

Claims24