Class / Patent application number | Description | Number of patent applications / Date published |
560037000 | The nitrogen is not bonded directly to a ring | 41 |
20080234508 | Process for the Preparation of N(5)-Ethylglutamine - Disclosed relates to a process for preparing N(5)-ethylglutamines economically without a specific purification process via a simplified and safe process, in which glutamic acid derivatives, represented by formula 1, protected by phthaloyl groups react with ethylamine to cause an amidation and a deprotection reaction in turn under the same reaction condition, thus preparing N(5)-ethylglutamines. | 09-25-2008 |
20090192326 | Preparation of sitagliptin intermediate - Intermediate compounds in the synthesis of Sitagliptin, 3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and amino protected-3-amino-4-(2,4,5-trifluorophenyl)but-2-enoic acid alkyl ester, and the stereoselective reduction of these compound to give Synthon I, or the amino-protected Synthon I, are provided. | 07-30-2009 |
20090281347 | METHOD FOR PRODUCING AMINO ACID PHOSPHATES - To provide a production method of phosphates of amino acids, typified by δ-aminolevulinic acid phosphate, or esters thereof. | 11-12-2009 |
20090306421 | NEW SYNTHESIS OF SUBSTITUTED HYDROXYMETHYL PHENOLS - The present disclosure relates to a process for the preparation of 2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol or its phenolic monoesters or salts thereof, characterized by the steps of a) reacting a compound of formula (II) with a mixture of a Grignard initiator and Mg in a solvent; b) optionally reducing the temperature of the Grignard reagent to a lower temperature than in step a), and reacting the resulting Grignard reagent with an excess of a carbonate in a solvent, to obtain a compound of formula (III) wherein A is a C | 12-10-2009 |
20100168460 | PROCESS FOR THE PREPARATION OF (2R,3S)-3-PHENYLISOSERINE METHYL ESTER ACETATE SALT - A process for the enantioselective preparation of (2R,3S)-3-phenylisoserine methyl ester acetate salt of formula (I) which is an useful building block for the synthesis of taxane derivatives. The process involves the resolution of racemic threo-phenylisoserine amide and its conversion into (I). | 07-01-2010 |
20110071310 | DIAMINO ACID DERIVATIVE STARTING MATERIAL, MANUFACTURING METHOD THEREOF, AND DIAMINO ACID DERIVATIVE MANUFACTURING METHOD - Provided is an efficient technology for synthesizing diamino acids (diamino acid derivatives). Disclosed is a manufacturing method for diamino acid derivatives wherein the fluorenyl groups of the diamino acid derivative starting materials represented by General Formula [II] or [IV] are removed. | 03-24-2011 |
20120004441 | METHOD OF ENANTIOSELECTIVE ADDITION TO IMINES - The present invention relates to a method of enantioselective addition to imines, including: reacting R | 01-05-2012 |
560038000 | The nitrogen is in same side chain as ester function | 28 |
20090054679 | PROCESS FOR PRODUCTION OF MONO-SUBSTITUTED ALKYLATED COMPOUND USING ALDIMINE OR DERIVATIVE THEREOF - The present invention provides a method for producing asymmetrical mono-substituted alkylated compounds of α-amino acids that are represented by a specific formula, using an aldimine-type Schiff base. In the method of the present invention, the process of alkylating an aldimine-type Schiff base in a medium in the presence of an optically-active quaternary ammonium salt phase-transfer catalyst and an inorganic base is initiated, and subsequently the reaction is quenched at a time earlier than a time for completion of the stoichiometric reaction of the alkylation reaction, so that a mono-substituted alkylated product with high optical purity can be obtained. | 02-26-2009 |
20100099907 | Methods of Synthesizing a Levodopa Ester Prodrug - Methods of synthesizing a levodopa ester prodrug, salts thereof, and synthetic intermediates thereof are disclosed. | 04-22-2010 |
20130079543 | METHOD FOR PRODUCING beta-AMINOCARBONYL COMPOUND - An optically active β-aminocarbonyl compound is obtained by a Mannich reaction between an aldimine in which: nitrogen is protected and a malonic acid diester, in the presence of optically active BINOL and dialkyl magnesium (in which two alkyl groups are the same or different) in an amount 1 to 2 molar times the amount of the BINOL. | 03-28-2013 |
20130204033 | ANTIPROLIFERATIVE COMPOUNDS, CONJUGATES THEREOF, METHODS THEREFOR, AND USES THEREOF - Antiproliferative compounds having a structure represented by formula (II), where n, R | 08-08-2013 |
20140288323 | CYCLOPROPENIMINE CATALYST COMPOSITIONS AND PROCESSES - The present invention provides, inter alia, a cyclopropenimine Brønsted base catalyst and a cyclopropenimine scaffold for use as a Brønsted base catalyst. This cyclopropenimine has the structure (100). Methods for making such a cyclopropenimine are also provided. Further provided are processes for carrying out an organic synthetic reaction and processes for catalyzing a proton transfer reaction enantioselectively using such a cyclopropenimine Brønsted base catalyst. | 09-25-2014 |
560039000 | Oxy in acid moiety | 15 |
20090082589 | ESTERS OF PENTAHYDROXYHEXYLCARBAMOYL ALKANOIC ACIDS - Provided are compounds of formula A and formula I: | 03-26-2009 |
20110015425 | PROCESS - The present invention relates to improved processes for the production of 2-amino-2-[2-(4-C | 01-20-2011 |
20120296109 | Levodopa Prodrugs, and Compositions and Uses Thereof - (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided. | 11-22-2012 |
20130090493 | PROCESS FOR THE PREPARATION OF ISOSERINE DERIVATIVES - This invention relates to a “one pot” process for the preparation of isoserine derivatives in high diastereoselective way. The process according to the invention includes the steps of reacting a protected glycidic acid with imines to yield isoserines protected both at the —OH and at the —COOH groups, deprotection of the obtained intermediates to isoserines or isoserine 1-4C— alkyl esters. Pure threo derivatives as the main isomer are obtained. | 04-11-2013 |
20140031577 | Haloalkylmethyleneoxyphenyl-Substituted Ketoenols - The invention relates to novel compounds of the formula (I), | 01-30-2014 |
20140046087 | Compound, Method for Producing the Same, and Method for Producing Oseltamivir Phosphate - A compound represented by the following general formula (1), and a method for producing the compound represented by the general formula (1), the method comprising: reacting together a compound represented by the following general formula (2), a compound represented by the following general formula (3), and a compound represented by the following general formula (4): | 02-13-2014 |
20140213813 | Haloalkylmethyleneoxyphenyl-Substituted Ketoenols - The invention relates to novel compounds of the formula (I), | 07-31-2014 |
20140213814 | Process For Extraction Of Peptides And Its Application In Liquid Phase Peptide Synthesis - A process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process includes a step a) and a step b): step a) including the addition of a component a1) and a component a2), whereby component a1) is toluene and component a2) is water, to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) including the subsequent separation of the organic layer containing the peptide from the aqueous layer. In an embodiment, a combination of toluene and an organic solvent 1 selected from n-heptane, 2-methyltetrahydrofuran, ethylacetate, isopropylacetate, acetonitrile and tetrahydrofuran is used for the process for extraction. The extraction step is preferably used in a process for preparation of a peptide in liquid phase. | 07-31-2014 |
20140350286 | Method for Making Two-Phase Solution of which Phase State Changes as aResult of Temperature Conversion React, and Apparatus for Implementing This - A method for making a number (N) of samples react under the same reaction conditions, wherein the samples have a solution where the phase state of a reaction solvent changes in a reversible manner between a two-phase solution state and a uniform solution state when the temperature fluctuates over or under a certain constant temperature, and the processes are carried out sequentially in the following steps: (A) the constant container heating step of heating a number of reaction containers simultaneously and maintaining the reaction containers at a predetermined temperature; (B) the sample heating step of putting a sample in each heated reaction container and of maintaining a two-phase solution at a predetermined temperature; (C) the reaction step of stirring the sample that has been heated to the predetermined temperature so as to gain a uniform solution, which is maintained for a predetermined period of time; (D) the cooling step of cooling the uniform solution without cooling the reaction container after the predetermined period of time has passed so as to gain a two-phase solution within the reaction container. | 11-27-2014 |
20150299104 | METHOD FOR PRODUCING 4-OXOQUINOLINE COMPOUND - The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2′): | 10-22-2015 |
20160176804 | METHODS OF SYNTHESIZING A LEVODOPA ESTER PRODRUG | 06-23-2016 |
560040000 | Phenylalanines | 4 |
20090137834 | LEVODOPA PRODRUGS, AND COMPOSITIONS AND USES THEREOF - Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed. | 05-28-2009 |
20090240074 | Process Of Making Optically Pure Melphalan - This invention provides a process of making 4-(bis-(2-hydroxyethyl)amino)-L-phenylalanine of the formula | 09-24-2009 |
20100197953 | LEVODOPA PRODRUGS, AND COMPOSITIONS AND USES THEREOF - Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed. | 08-05-2010 |
20100222608 | SYNTHESIS OF N-[N-(3,3-DIMETHYLBUTYL)-L-ALPHA-ASPARTYL]-L-PHENYLALANINE 1-METHYL ESTER USING 3,3-DIMETHYLBUTYRALDEHYDE PRECURSORS - N—[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester is produced by hydrogenation of L-α-aspartyl-L-phenylalanine 1-methyl ester and 3,3-dimethylbutyraldehyde produced in situ by the hydrolysis or cleavage of a 3,3-dimethylbutyraldehyde precursor. The production method is efficient and low cost, as compared with conventional N—[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester synthesis. | 09-02-2010 |
560041000 | Amide in acid moiety | 8 |
20080293962 | Novel compounds of the N-acylamino amide family compositions comprising them and uses thereof - The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure for tissues. | 11-27-2008 |
20090030227 | Polyisocyanide Derivative Having Controlled Helical Main Chain Structure - The object is to provide: a method for producing a polymer having a stable right-handed or left-handed helical structure from a single type of monomer in a per-selective manner and controlling the proportion between a polymer having the right-handed helical structure and a polymer having the left-handed helical structure; and a polymeric material which can be used for the formation of any of the right-handed and left-handed helical structures. Thus, disclosed are: a method for production of a polyisocyanide derivative having a stable helical main chain structure with a right-handed or left-handed helix or a mixture thereof from a single type of monomer by polymerizing an aromatic isocyanate having a substituent harboring a structure —CONH in the aromatic ring and a hydrophobic moiety having 6 or more carbon atoms in a polymerization solvent, wherein the direction of the helix depends on the polarity of the polymerization solvent; a poly(aromatic isocyanide) derivative produced by the method; and an aromatic isocyanide which is useful as a monomer for use in the production of the poly(aromatic isocyanide) derivative. | 01-29-2009 |
20120016151 | PROCESS FOR MANUFACTURE AND RESOLUTION OF 2-ACYLAMINO-3-DIPHENYLPROPANOIC ACID - The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors. | 01-19-2012 |
20120203023 | Process For Preparing A Phenylalanine Derivative - A novel process for the preparation of a phenylalanine derivative of formula (I): | 08-09-2012 |
20130109880 | PHENYL-N-ACYL DERIVATIVES OF AMINES AND AMINO ACIDS, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL COMPOSITION AND USE THEREOF | 05-02-2013 |
20140179947 | PROCESS FOR MANUFACTURE AND RESOLUTION OF 2-ACYLAMINO-3-DIPHENYLPROPANOIC ACID - The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors. | 06-26-2014 |
20150073172 | SYNTHESIS OF DIAMIDO GELLANTS BY USING DANE SALTS OF AMINO ACIDS - The invention relates to a method for the synthesis of a compound according to formula I comprising the following steps: a) reacting a Dane salt according to formula II and a Dane salt according to formula III with a coupling reagent; b) adding a diamine according to formula IV to the reaction mixture; and c) adding an acid to the reaction mixture to adjust the pH value of the reaction to <7; wherein L represents a C | 03-12-2015 |
20150073173 | LYSINE-GLUTAMIC ACID DIPEPTIDE DERIVATIVES - The invention relates to compounds of the formula | 03-12-2015 |
560042000 | Oxy in acid moiety | 6 |
20090247781 | SYNTHESIS OF PHENOXYACETIC ACID DERIVATIVES - The present invention relates to an improved process for the preparation of substituted 2-(4-carbonylmethoxy-optionally 2,5-disubstituted-phenyl-acetaldehydes, in particular 2-(4-alkoxycarbonylmethoxy-optionally 2,5-disubstituted-phenyl)-acetaldehydes and their use in the synthesis of optionally substituted 2-[4-[2-[[-2-hydroxy-2-(4-hydroxyphenyl)- | 10-01-2009 |
20100113820 | INHIBITORS OF ALPHA4 MEDIATED CELL ADHESION - The present invention relates to a phenylalanine derivative of Formula (I) wherein X | 05-06-2010 |
20110105783 | PROCESS FOR THE PREPARATION OF FESOTERODINE - A process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine), its (S)-enantiomer, and novel intermediates useful in thei synthesis. | 05-05-2011 |
20110263888 | Cycloalkylmethylamines - The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications. | 10-27-2011 |
20130345466 | CRYSTALLINE FORMS OF A 3-CARBOXYPROPYL-AMINOTETRALIN COMPOUND - The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms. | 12-26-2013 |
20150094485 | PROCESS FOR THE PREPARATION OF OPTICALLY PURE FESOTERODINE DERIVATIVES - 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, can be produced by treating a compound of formula (II) with a chiral alcohol to yield the diastereomeric esters of formula (IV) and (IV′), which can be further transformed into a compound of formula (I), or an enantiomer, solvate or salt thereof, wherein R1 is C1-C8 alkyl; and R2 and R3, independently of one another, represent H or C1-C6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound. | 04-02-2015 |