| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 21 | DEPROTECTION METHOD FOR PROTECTED HYDROXYL GROUP | US14057384 | 2013-10-18 | US20140058113A1 | 2014-02-27 | Yuichiro Ishibashi; Yasushi Matsumura |
| To deprotect an alcoholic hydroxyl group protected by a t-butyldimethylsilyl group without influencing a functional group unstable to an acid. In the presence of a solvent, an alcohol having a hydroxyl group protected by a t-butyldimethylsilyl group is deprotected in the presence of an acid or an acid salt having a pKa of from 1.0 to 3.0 in water. | ||||||
| 22 | METHOD FOR PRODUCING PEPTIDE | US13122850 | 2009-10-06 | US20120004457A1 | 2012-01-05 | Hironobu Hojo; Yoshiaki Nakahara |
| An object of the present invention is to provide a novel method for producing a peptide utilizing a ligation reaction in which ligation efficiency is excellent and side reactions to other functional groups in the peptide are hard to occur, in comparison with the conventional native chemical ligation methods utilizing the thiol auxiliary group. The present invention provides a method for producing a peptide which comprises a step of causing a first peptide and a second peptide to react in the presence of a reducing agent to obtain a ligated product of the first peptide and the second peptide, wherein the first peptide contains, at the C-terminal end, an amino acid derivative having a thioester group, and the second peptide contains, at the N-terminal end, a serine or threonine derivative having a thiol auxiliary group. | ||||||
| 23 | METHOD FOR PRODUCING OPTICALLY ACTIVE AMINO ACID DERIVATIVE | US12993661 | 2009-06-02 | US20110166354A1 | 2011-07-07 | Shohei Yamamoto; Akio Fujii; Masaru Mitsuda |
| The present application relates to a method for producing an optically active α-amino acid derivative, comprising steps of reacting an α-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active α-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity. | ||||||
| 24 | SOLVENT-FREE SYNTHESIS OF AMPHIPHILIC POLYMERIC MATERIAL | US12733698 | 2008-10-15 | US20100233314A1 | 2010-09-16 | Terence Cosgrove; Roger Pettman; Erol Hasan |
| The present invention provides a method for making a composition comprising an amphiphilic polymeric material which comprises a straight or branched chain carbon-carbon backbone and a multiplicity of side chains attached to the backbone; wherein in the method, backbone precursors comprising acylating groups are mixed with side chain precursors which comprise a nucleophilic group at at least one terminus, to form a reaction mixture; the backbone precursors, side chain precursors and/or the reaction mixture are heated; the reaction mixture is stirred; and the nucleophilic groups react with the acylating groups to form the amphilphilic polymeric material wherein the side chains are linked to the backbone via acyl linkages; characterised in that the reaction mixture does not comprise organic solvent. | ||||||
| 25 | Fluorous tagging and scavenging reactants and methods of synthesis and use thereof | US11338378 | 2006-01-24 | US20060128957A1 | 2006-06-15 | Wei Zhang; Zhiyong Luo |
| The present invention includes methods and compositions for increasing the fluorous nature of an organic compound by reacting it with at least one fluorous compound to produce a fluorous tagged organic compound. The increased fluorous nature of the fluorous tagged organic compound can then be utilized to separate the fluorous organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom. The resultant fluorous tagged organic compound can be subjected to subsequent chemical transformations, wherein the fluorous nature of the tagged compound is utilized to increase the ease of separation of the fluorous tagged organic compound from untagged reagents, reactants, catalysts and/or products derived therefrom, after each chemical transformation. The chemical transformations result in a second fluorous tagged organic compound wherein the fluorous nature of the second fluorous tagged organic compound can then be reduced by removing the fluorous group therefrom, thereby producing a second organic compound that may be employed as a pharmaceutical compound or intermediate, or a combinatorial library component. | ||||||
| 26 | Process for preparation of (R)-1- (aryloxy)propan-2-ol | US09839062 | 2001-04-20 | US06448449B2 | 2002-09-10 | Jay Francis Larrow |
| A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol, which is a useful intermediate in the synthesis of the widely used antibiotic Levofloxacin is provided. A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-2-trimethylsiloxypropane is also described. The process includes the ring opening of (R)-propylene oxide with 2,3-difluoro-6-nitrophenyl trimethylsilyl ether in the presence of an optically active Co(salen) catalyst. The trimethylsilyl group of the reactant is transferred to the product aryloxy alcohol, which serves to protect the secondary alcohol in situ. Upon isolation, the trimethylsilyl group is removed and the resulting regioisomeric mixture purified to yield the desired (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol in high purity and yield. | ||||||
| 27 | Process for preparation of (R)-1- (aryloxy)propan-2-ol | US09839062 | 2001-04-20 | US20020007090A1 | 2002-01-17 | Jay Francis Larrow |
| A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol, which is a useful intermediate in the synthesis of the widely used antibiotic Levofloxacin is provided. A process for the preparation of (R)-1-(2,3-difluoro-6-nitrophenoxy)-2-trimethylsiloxypropane is also described. The process includes the ring opening of (R)-propylene oxide with 2,3-difluoro-6-nitrophenyl trimethylsilyl ether in the presence of an optically active Co(salen) catalyst. The trimethylsilyl group of the reactant is transferred to the product aryloxy alcohol, which serves to protect the secondary alcohol in situ. Upon isolation, the trimethylsilyl group is removed and the resulting regioisomeric mixture purified to yield the desired (R)-1-(2,3-difluoro-6-nitrophenoxy)-propan-2-ol in high purity and yield. | ||||||
| 28 | METHOD FOR PRODUCING CHIRAL AMINONITRILES | US16328519 | 2017-08-17 | US20190185428A1 | 2019-06-20 | Harald GRÖGER; Tobias BETKE; Philipp ROMMELMANN |
| The invention relates to a method for preparing an N-acyl- or N-sulfonyl-α-aminonitrile, comprising the following steps: a) condensation of an N-acyl- or N-sulfonyl-α-aminoaldehyde with hydroxylamine to give an aldoxime, and b) dehydration of the aldoxime obtained in step a) to give an N-acyl- or N-sulfonyl-α-aminonitrile. In an advantageous manner, the absolute configuration can be retained in the conversion to the N-acyl- or N-sulfonyl-α-aminonitrile. | ||||||
| 29 | Novel Process for the Preparation of Tavaborole, Its Novel Polymorphic Forms and the Polymorphs Thereof | US16094470 | 2016-07-21 | US20190119306A1 | 2019-04-25 | Manik Reddy PULLAGURLA; Mecheril Valsan NANDA KUMAR; Bhasakar Reddy PITTA; Jagadeesh Babu RANGISETTY |
| The invention relates to novel process for preparation of Tavaborole. The invention also relates to novel polymorphic forms of Tavaborole and process for preparation of those polymorphic forms. The invention also relates to process for purification of Tavaborole to obtain the Tavaborole in significantly high yield and substantially pure form. | ||||||
| 30 | AN IMPROVED PROCESS FOR THE PREPARATION OF LACOSAMIDE | US16076486 | 2017-06-12 | US20190047944A1 | 2019-02-14 | Dhananjay D. SATHE; Arijit DAS; Sanjay RAIKAR; Rahul BHAGWATKAR; Ramdas AHIRE |
| The present invention relates to an improved process for the synthesis of (R)-Lacosamide in which free base of O-methyl-N-benzyl-D-Serinamide is not isolated before acylation. The process avoids the use of column chromatography and chiral resolution for the preparation of different stages of Lacosamide. | ||||||
| 31 | Process for preparing ixazomib citrate and intermediates therefor | US15860949 | 2018-01-03 | US10118937B1 | 2018-11-06 | Tsung-Yu Hsiao; Jyh-Hsiung Liao |
| A process for making ixazomib citrate of formula VI comprising reacting a compound of formula V with citric acid to form ixazomib citrate of formula VI: wherein R is hydrogen or an amide protecting group. | ||||||
| 32 | SUBSTITUTED BENZOTRIAZOLE PHENOLS | US15741647 | 2016-06-30 | US20180186757A1 | 2018-07-05 | Kelly A. Volp; Nathan E. Schultz; Fuming B. Li |
| Benzotriazole phenols with substituents either ortho to the phenol hydroxyl group and/or para to the phenol hydroxyl group can be prepared from the unsubstituted benzotriazole phenol by coupling reactions. The ortho substituent group can be a simple alkoxy or amino group, or the ortho substituent group can be a linking group, linking the benzotriazole phenol to another benzotriazole phenol group. | ||||||
| 33 | PROCESS FOR PREPARATION OF DAPAGLIFLOZIN | US15571112 | 2016-05-04 | US20180127391A1 | 2018-05-10 | Shekhar Bhaskar Bhirud; Kumar Hari BHUSHAN; Raghu Ram SURAPARAJU; Nandkumar GAIKWAD; Sharad GORE; Rajendra JAGDHANE; Mandar KULKARNI |
| The present invention relates to a process for the preparation of amorphous dapagliflozin. The present invention relates to 2,3-butanediol solvate of dapagliflozin and process for its preparation. | ||||||
| 34 | AGENT FOR INTRODUCING PROTECTING GROUP FOR HYDROXY GROUP AND/OR MERCAPTO GROUP | US15517899 | 2015-09-30 | US20170305809A1 | 2017-10-26 | Kohei Torikai |
| A novel agent for introducing a protecting group for a hydroxy group and/or a mercapto group that can be introduced and removed under mild conditions is provided. The agent for introducing a protecting group for a hydroxy group and/or mercapto group of a substrate compound having the hydroxy group and/or mercapto group is represented by the following formula (I), wherein A represents a ring structure having 1 to 5 rings in which two carbon atoms of an adjacent benzene ring are included, the ring structure comprises a substituted or unsubstituted five-membered ring or six-membered ring and optionally include a heterocycle; each of R1, R2, R3, and R4 is independently a hydrogen atom or a linear or branched alkyl group having 1 to 5 carbon atoms; and X is a halogen atom or OSO2R5 (R5=an aryl group or an alkyl group). | ||||||
| 35 | METHOD FOR PRODUCING 2-AMINO-SUBSTITUTED BENZALDEHYDE COMPOUND | US15504499 | 2015-08-25 | US20170226046A1 | 2017-08-10 | Shinichi KOBAYASHI |
| The present invention provides a method for producing a benzaldehyde in which an amino group is bonded in the 2 position, a halogeno group or an alkoxy group is bonded in the 3 position, and a hydrogen atom, an alkyl group, a halogeno group, an alkoxy group, or a cyano group is bonded independently in each of the 4, 5, and 6 positions, the method including: preparing a benzaldehyde in which a halogeno group or an alkoxy group is bonded in the 3 position, a hydrogen atom is bonded in the 2 position, and a hydrogen atom, an alkyl group, a halogeno group, an alkoxy group, or a cyano group is bonded independently in each of the 4, 5, and 6 positions so that a lithiation reaction is most active at the 2 position; acetal-protecting a formyl group in the benzaldehyde; sequentially performing lithiation, azidation, and amination of the 2 position; and the performing acetal deportection. | ||||||
| 36 | Amino acid generator and polysiloxane composition containing the same | US13941890 | 2013-07-15 | US09257576B2 | 2016-02-09 | Taku Kato; Junpei Kobayashi; Satoko Takano; Naoki Sakumoto |
| A coating film forming composition includes an amino acid generator including a protecting group that is eliminated to generate an amino acid. A coating film forming composition includes a component (A): the amino acid generator; a component (B): a hydrolyzable silane, a hydrolysis product thereof, a hydrolysis-condensation product thereof, or a mixture thereof; and a component (C): a solvent. | ||||||
| 37 | Hydroxy group protecting agent and hydroxy group protection method | US14359183 | 2012-11-16 | US09126954B2 | 2015-09-08 | Munetaka Kunishima; Hikaru Fujita; Kohei Yamada |
| To provide: a hydroxy group protecting agent which is stable and easy to use, does not have carcinogenicity, a tearing property or the like, and is inexpensive; and a hydroxy group protection method which enables the protection of a hydroxy group under acidic conditions.[Solution] A hydroxy group protecting agent in which at least one protecting group is bound to a nitrogen-containing electron-withdrawing heterocyclic ring through any one of an oxygen atom, a sulfur atom and a nitrogen atom. The heterocyclic ring is a triazine ring or the like, and the protecting group is a benzyl group or the like. Specifically, the hydroxy group protecting agent is 2,4,6-tribenzyloxy-1,3,5-triazine, 2,4,6-tris(4-methoxybenzyloxy)-1,3,5-triazine or the like. In addition, 2,4,6-tris(t-butoxy)-1,3,5-triazine or the like can also be used. For protecting a hydroxy group, a compound of interest which has a hydroxy group is reacted with the hydroxy group protecting agent under acidic conditions. | ||||||
| 38 | Processes for removal of dibenzofulvene | US13020838 | 2011-02-04 | US08703912B2 | 2014-04-22 | Yuji Nishiuchi; Terutoshi Kimura |
| A dibenzofulvene amine adduct is removed by contacting a reaction mixture containing the dibenzofulvene amine adduct, which is obtained by reacting, for deprotection, an amino acid compound protected with an Fmoc group with an amine compound containing a nitrogen atom which is bonded to at least one hydrogen atom, with carbon dioxide, and removing the carbonate of the dibenzofulvene amine adduct. Alternatively, a dibenzofulvene amine adduct is removed by mixing a reaction mixture during a deprotection reaction of the amino acid compound protected with an Fmoc group, or after the reaction with an amine compound containing a nitrogen atom which is bonded to at least one hydrogen atom to give a mixture containing the dibenzofulvene amine adduct, contacting the mixture with carbon dioxide, and removing the carbonate of the dibenzofulvene amine adduct. | ||||||
| 39 | AMINO ACID GENERATOR AND POLYSILOXANE COMPOSITION CONTAINING THE SAME | US13941890 | 2013-07-15 | US20130313669A1 | 2013-11-28 | Taku KATO; Junpei KOBAYASHI; Satoko TAKANO; Naoki SAKUMOTO |
| A coating film forming composition includes an amino acid generator including a protecting group that is eliminated to generate an amino acid. A coating film forming composition includes a component (A): the amino acid generator; a component (B): a hydrolyzable silane, a hydrolysis product thereof, a hydrolysis-condensation product thereof, or a mixture thereof; and a component (C): a solvent. | ||||||
| 40 | AMINO ACID GENERATOR AND POLYSILOXANE COMPOSITION CONTAINING THE SAME | US12993700 | 2009-05-19 | US20110073977A1 | 2011-03-31 | Taku Kato; Junpei Kobayashi; Satoko Takano; Naoki Sakumoto |
| There is provided an amino acid generator comprising a protecting group for an amino group that is eliminated to generate an amino acid, and a coating film forming composition using the amino acid generator and a polysiloxane composition containing the amino acid generator. A coating film forming composition comprising: a component (A): an amino acid generator comprising a protecting group that is eliminated to generate an amino acid, which is a compound of Formula (1): D-A (1) where D is a protecting group for an amino group, and A is an organic group remaining after subtracting hydrogen atoms from an amino group of an amino acid; a component (B): a hydrolyzable silane, a hydrolysis product thereof, a hydrolysis-condensation product thereof, or a mixture thereof; and a component (C): a solvent. | ||||||
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