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Class 562/402 - Physical resolution


Subclass of Class 562 - Organic compounds -- part of the class 532-570 series
Definition: Processes wherein the separation is performed solely by
No. of patents: 96
Last issue date: 03/16/2010


1      
NumberTitleIssue Date
7678938Optical resolution of 3-carbamoylmethyl-5-methyl hexanoic acid
The invention relates to pure (R)-CMH and to the optical resolution of CMH-racemate, a key intermediate in the synthesis of (S)-Pregabalin. The invention also relates to the process for optically purifying (R)-CMH and to the process for isolating (S)-CMH from the mo...
03/16/2010
7321055Production method of optically active dephenylalanine compounds
Optically active diphenylalanine compounds may be conveniently prepared in a good yield by reacting a diphenylalanine compound represented by formula (1) with an optically active amine compound represented by formula (2) in the presence of an organic solvent to give...
01/22/2008
7214819Fluorous triphasic reaction and separation processes for the generation of enantioenriched alcohols, amines, carboxylic acids and related compounds
A method of obtaining an enantioenriched organic compound comprising the steps of: 1) generating from a starting racemic, non-enantiopure or achiral compound a first mixture comprising at least one fluorous-tagged compound and at least one other non-fluorous tagged ...
05/08/2007
7214820Process for producing optically active flurbiprofen
The present invention provides a method for producing optically active flurbiprofen. The method of the present invention includes mixing racemic flurbiprofen and (S)- or (R)-3-methyl-2-phenylbutylamine in an organic solvent to produce a diastereomeric salt; and trea...
05/08/2007
7034178Process for the production of 3-phenylisoserine
This invention is drawn to a process for the production of (R,R)-phenylisoserine or a 1–4C-alkyl ester thereof. ...
04/25/2006
7019152Process for the optical resolution of a precursor of sclareolide
The present invention relates to the field of organic synthesis and more particularly to a new process for the optical resolution of a precursor of sclareolide. This process includes the reaction of [(1RS,2RS,4aSR,8aSR)-2-hydroxy-2,5,5,8a-tetramethyldecahydronaphtha...
03/28/2006
6939515Apparatuses and methods for creating and testing pre-formulations and systems for same
The invention provides methods, apparatus, and systems for performing high-throughput preparation and screening of salts and polymorphs of drug candidates. The invention is directed towards enhancing the pre-formulation discovery process used for drug development. I...
09/06/2005
6559338Method for racemate splitting of 2-hydroxypropionic acids
A process for racemate resolution of 2-hydroxypropionic acids by reacting the racemic acid with an optically active base and subsequently separating off a diastereomeric salt of acid and base comprises using 1-(4-chlorophenyl)ethylamine as optically activ...
05/06/2003
6462229Process for the preparation of (-)-଱-(difluoromethyl)ornithine-monohydrochloride monohydrate
(&#b1;)-଱-(Difluoromethyl)-ornithine is separate into its isomers using (-)-O,O'-di-p-toluoyl-L-tartaric acid. (-)-଱-(Difluoromethyl)-ornithine monohydrochloride monohydrate and in particular the (-)-isomer are inhibitors of ornithine decarbox...
10/08/2002
6462221Synthesis of nitroalcohol diastereomers
The present invention relates to a method of preparing a 1-nitro-3-substituted-3-amino-2-propanol diastereomer represented by Structural Formula I: ##STR1## In Structural Formula I, R is an amine protecting group, and R1 is an amino acid s...
10/08/2002
6458955Process for preparation of pharmaceutically desired enantiomers
Improved processes for preparation of high enantiomeric purity compounds center on resolution using simulated moving bed chromatography of a racemic precursor early in the synthesis. Resolution is effected with high enantiomeric purity, and subsequent rea...
10/01/2002
6342629Process for production of optically active n-protected-n-methyl-phenylalanine derivative
There is provided a process for industrially and efficiently producing an optically active N-protected-N-methyl-4-halogenophenylalanine at a high purity, which is useful as an intermediate for the production of pharmaceutical agents. An optically active N...
01/29/2002
6207854Preparation of 3-amino-3-cyclopropylpropanoate esters
Disclosed a process for preparing substantially enantiomerically pure 3-amino-3-cyclopropylpropanoate esters, i.e., esters of 3-amino-3-cyclopropylpropanoic acid (3-cyclopropylalanine esters or 3-CPA esters) by a 5-step process wherein cyclopropanecarboxa...
03/27/2001
6147254Process for resolving mixtures of carbocyclic stereoisomers
A process for the preparation of carbocyclic stereoisomers of formulae (I), (I'), (IIA'), (IIB'), (VA') and (VB'), including enantiomerically pure (IIA'), (I) and (I') utilizing fractional crystallization of salts formed with a chiral base; a reducing age...
11/14/2000
6093846Process for preparing optically active 2-hydroxy-methyl-3-phenylpropionic acid
A process for preparing optically active 2-hydroxymethyl-3-phenylpropionic acid by resolving (RS)-2-hydroxymethyl-3-phenylpropionic acid via crystallization of an optically active amine salt, where the amine is optically active cis-1-amino-2-indanol salt,...
07/25/2000
6090971Resolution process for cyclohexylphenyl glycolic acid
A process for the preparation of optically active phenylcyclohexylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)-- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargy...
07/18/2000
6087530Process for preparing ଲ-amino-଱-hydroxy acid derivatives
An object of the present invention is to provide a process for producing a ଲ-amino-଱-hydroxy acid derivative via efficient and industrially utilizable steps. The present invention provides a process for producing a ଲ-amino-଱-hydrox...
07/11/2000
6008403Method for producing optically active amino acid of derivative thereof having high optical purity
A method for producing an optically active amino acid or derivative thereof having a high optical purity from an optically active amino acid comprising optical isomers or derivative thereof, which comprises any one of processes (A), (B), and (C), wherein ...
12/28/1999
5994560Resolution of racemic mixtures using polymers containing chiral units
Described herein is a novel process to resolve a racemic compound into its optically active isomers without need for chemical transformation such as salt formation. The process advantageously utilizes polymers containing chiral moieties in their repeat un...
11/30/1999
5892112Process for preparing synthetic matrix metalloprotease inhibitors
Synthetic mammalian matrix metalloprotease inhibitors are disclosed that are useful for treating or preventing diseases wherein said diseases are caused by unwanted mammalian matrix metalloprotease activity and include skin disorders, keratoconus, resteno...
04/06/1999
5840964Process for the preparation of the enantiomers of 2-(2-fluoro-4-biphenyl)propionic acid
A process for the preparation of 2-(2-fluoro-4-biphenyl)propianic acid enantiomers comprising a II order resolution of ketals of formula ##STR1## wherein R1 ad R2 have the meanings reported in the description; the asterisk shows...
11/24/1998
5763647Preparation of optically active 1,4-bridged-cyclohexane carboxylic acid derivatives
A process for preparing an optically active 1,4-bridged-cyclohexane carboxylic acid derivatives which are clinically important thromboxane A2 thromboxane of formula (IV): ##STR1## wherein, R is phenyl or phenyl substituted with hydroxy, lo...
06/09/1998
5739383Resolution of racemic mixtures using polymers containing chiral units
Described herein is a novel process to resolve a racemic compound into its optically active isomers without need for chemical transformation such as salt formation. The process advantageously utilizes polymers containing chiral moieties in their repeat un...
04/14/1998
5721103Trienoic retinoid compounds and methods
Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use....
02/24/1998
5510520Optical resolution method
The present invention provides three optical resolution methods. The first aspect comprises the steps of adding an optically active bifunctional resolving reagent to a bifunctional compound to form a liquid material, precipitating crystals therefrom, and ...
04/23/1996
5449728Optically active acetylene polymer, membrane thereof and optical resolution method using the same
An optically active acetylene polymer which is obtained by polymerizing an optically active form of 1-[dimethyl(10-pinanyl)silyl]-1-propyne which is represented by the following formula (I) and has a weight-average molecular weight of from 10,000 to 1,000...
09/12/1995
5426215Process for converting [R(-)-2(3-benzoylphenyl)-propionic acid to the S(+) isomer]
Process for transforming (benzoyl-3-phenyl)-2-propionic-R(-) acid into an S(+) isomer through the action of a base either in situ during the splitting of racemic ketoprofen or on the crystallization mother liquor of a (benzoyl-3-phenyl)-2-propionic-S(+) a...
06/20/1995
5395962Optical resolution method
The present invention provides three optical resolution methods. The first aspect comprises the steps of adding an optically active bifunctional resolving reagent to a bifunctional compound to form a liquid material, precipitating crystals therefrom, and ...
03/07/1995
5391634Optically-active, amphiphilic, water-soluble free-radical addition copolymers and their use in the resolution of racemic mixtures
Optically-active, amphiphilic, free-radical addition copolymers having an optically-active hydrophobic portion and an ionic hydrophilic portion are effective resolving agents. This utility is based on a unique combination of properties, viz., water solubi...
02/21/1995
5321154Optical resolution of (&#b1;)-2-(4-isobutylphenyl)-propionic acid
(&#b1;)-2-(4-Isobutylphenyl)-propionic acid can be resolved into optically active isomers easily and with high yields. The method is characterized by the use of the optically active amine of the following general formula (I) or (II) as a resolving agent. ...
06/14/1994
5306826Process for preparation of an optically active amino acid amide
The present invention relates to a process for the preparation of optically active amino acid amide. L-amino and D-amino acid amides are mixed in the presence of 0.5-4 equivalents of an aldehyde, relative to the quantity of amino acid amide, in the presen...
04/26/1994
5302751Profen resolution
A process is disclosed that is useful for separating the enantiomers of a racemic mixture of an aliphatic carboxylic acid having the formula ##STR1## where R1 is hydrogen or alkyl, R2, R3 and R4 are indepen...
04/12/1994
5302741Optical resolution of threo-2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)-propionic acid
D(+)-threo-2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, an important intermediate in the synthesis of diltiazem hydrochloride, is obtained in better yields and high optical purity by a novel resolution process comprising the reaction...
04/12/1994
5231181Process for the preparation of (8As,12AS,13AS)-decahydroisoquino ((2,1-G) (1,6)-naphthyridin-8-one derivatives
The invention provides a process for preparing single enantiomers of compounds represented by the formula: ##STR1## and chiral acid addition salts thereof; wherein: X and Y are independently hydrogen; lower alkyl; lower alkoxy; or halo; or X and Y ta...
07/27/1993
5200555Process for the preparation of S(+)-6-methoxy-଱-methyl-2-naphthalene-acetic acid
The invention relates to a process for the preparation of S(+)-6-methoxy-଱-methyl-2-naphthalene-acetic acid by resolution of R,S-6-methoxy-଱-methyl-2-naphthalene-acetic acid. According to the invention R,S-6-methoxy-଱-methyl-2-naphthalen...
04/06/1993
5198557Process for the resolution of 3-(4-substituted-phenyl)-glycidic acid derivatives
A process for the kinetic resolution of cis or trans enantiomeric mixtures of the compounds of formula ##STR1## wherein R3 and X have the meanings reported in the specification and the asterisks mark the asymmetric carbon atoms, is describ...
03/30/1993
5196575Supercritical separation of isomers of functional organic compounds at moderate conditions
A method of separating isomers of functionalized aromatic compounds using solvent-modified supercritical carbon dioxide is disclosed and claimed. In one embodiment, isomers of hydroxynaphthoic acid are separated by selective extraction of the more soluble...
03/23/1993
5191112Process for optical resolution of (&#b1;)-2-(3-benzoyl)-phenylpropionic acid
Optical resolution of (&#b1;)-2-(3-benzoyl)-phenylpropionic acid is attained effeciently in high yield by the use of a specific optically active amine which is represented by the general formula [I]: ##STR1## wherein R1 either stands for a...
03/02/1993
5189208Ibuprofen resolution
A process for obtaining a substantially pure enantiomer of ibuprofen is described. The process utilizes first an enantiomerically enriched mixture of ibuprofen obtained from kinetic resolution, diastereomeric crystallization or asymmetric synthesis proces...
02/23/1993
5183922Process for the optical resolution of threo-2-hydroxy-3-(2'-aminophenylthio)-3-(4"-methoxyphenyl)-propionic acid
The present invention relates to a process for the separation of the enantiomers of threo-2-hydroxy-3-(2'- aminophenylthio)-3-(4"-methoxyphenyl)-propionic acid, which is an important intermediate in the synthesis of pharmacologically active compounds...
02/02/1993
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