Abstract: The present invention relates to a novel process for the preparation of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I:
The method comprises of the TEMPO oxidation of a primary alcohol of 3-O-protected-2-hydroxymethyl-6-alkyl-4H-pyran-4-one of formula III to 3-O-protected-6-alkyl-4-oxo-4H-pyran-2-carboxylic acid of formula II. Reaction of compound of formula II with methylamine and 1,1-carbonyldiimidazole in an inert solvent affords 3-O-protected-N, 1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide, which is deprotected to give of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I.
Abstract: The present invention relates to a novel process for the preparation of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I:
The method comprises of the TEMPO oxidation of a primary alcohol of 3-O-protected-2-hydroxymethyl-6-alkyl-4H-pyran-4-one of formula III to 3-O-protected-4-alkyl-4-oxo-4H-pyran-2-carboxylic acid of formula II. Reaction of compound of formula II with methylamine and 1,1-carbonyidiimidazole in an inert solvent affords 3-O-protected-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide, which is deprotected to give of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I.
Abstract: The present invention relates to a novel process for the preparation of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I:
The method comprises of the TEMPO oxidation of a primary alcohol of 3-O-protected-2-hydroxymethyl-6-alkyl-4H-pyran-4-one of formula III to 3-O-protected-6-alkyl-4-oxo-4H-pyran-2-carboxylic acid of formula II. Reaction of compound of formula II with methylamine and 1,1-carbonyldiimidazole in an inert solvent affords 3-O-protected-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide, which is deprotected to give of 3-hydroxy-N,1,6-trialkyl-4-oxo-1,4-dihydropyridine-2-carboxamide of formula I.
Abstract: A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate) has been obtained. Preparation of the novel form of azithromycin comprises the steps of dissolving azithromycin in isopropanol, followed by the slow addition of water to the organic solution.
Abstract: Novel process for the preparation of quinolone carboxylic acid derivatives of general formula I, and intermediates thereof as illustrated in Scheme 1 wherein the key intermediate is a compound of formula IX.
Type:
Grant
Filed:
March 11, 1998
Date of Patent:
June 22, 1999
Assignee:
Apotex, Inc.
Inventors:
Ian Egle, Regis C.S.H. Leung-Toung, Bo Lei, Tim Fat Tam, Tao Xin, Khashayar Karimian
Abstract: A process for preparing pure amorphous cefuroxime axetil comprising the steps of dissolving crystalline cefuroxime axetil in a highly polar organic solvent and adding the resulting solution to water, or alternatively, dissolving crystalline cefuroxime axetil in a highly polar solvent and adding small quantities of water to the organic solution and adding the resulting organic-aqueous solution to water.
Abstract: The invention relates to a novel process to prepare 1,4-dihydropyridines and in particular amlopidine and in novel intermediates obtained during the synthesis of the 1,4-dihydropyridines which have potential activity as antihypertensive agents.
Type:
Grant
Filed:
October 10, 1996
Date of Patent:
March 3, 1998
Assignee:
Apotex, Inc.
Inventors:
Regis Chung Soon Hin Leung-Toung, Khashayar Karimian, Tim Fat Tam
Abstract: A novel microorganism, Penicillium adametzioides and a process of using the microorganism to produce compactin, the process consisting of fermentation in a nutrient medium.
Type:
Grant
Filed:
September 19, 1996
Date of Patent:
November 25, 1997
Assignee:
Apotex, Inc.
Inventors:
Scott Primrose, David King, Ed Yaworski, Jayaramaiyer Radhakrishnan, David He, Xinfa Xiao
Abstract: A pill guide for use in combination with pill, capsule and caplet dispensing trays has a tapered guide channel for removable attachment to the pill return outlet of the tray. The guide combines with adjacent wall portions of the tray return outlet to form a convergent funnel, through which unwanted pills may be discarded back to the bulk supply from where they came. The pill guide may incorporate a guidance lip to facilitate alignment of the tray with the bulk receptacle.
Abstract: A novel microorganism, Coniothyrium fuckelii ATCC 74227, and a process of using the microorganism for the production of lovastatin comprising fermenting Coniothyrium fuckelii ATCC 74227 or a lovastatin-producing mutant thereof in a nutrient medium containing assimilable sources of carbon, nitrogen, and inorganic salts under aerobic fermentation conditions.
Abstract: A process is disclosed for the preparation of simvastatin and its analogs through a novel intermediate (III), which enables a selective .alpha. carbon alkylation of the C-8 acyl side chain.
Type:
Grant
Filed:
November 8, 1993
Date of Patent:
February 28, 1995
Assignee:
Apotex, Inc.
Inventors:
Rudolf Kubela, Jayaramaiyer Radhakrishnan
Abstract: A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate) has been obtained. Preparation of the novel form of azithromycin comprises the steps of dissolving azithromycin in isopropanol, followed by the slow addition of water to the organic solution.