公开(公告)号：US20180305301A1

公开(公告)日：2018-10-25

申请号：US16024088

申请日：2018-06-29

Applicant: Politechnika Warszawska

Inventor： Krzysztof BUJNOWSKI ,  Ludwik SYNORADZKI ,  Jerzy WISIALSKI ,  Agnieszka KROLIKOWSKA ,  Jacek BORDZILOWSKI ,  Marcin KOZIOROWSKI ,  Roman ZADROZNY ,  Anna JERZAK ,  Krzysztof DZIENIS

IPC: C07C249/04 ,  C23F11/14 ,  C09D5/08 ,  C07C249/08 ,  C08K5/33 ,  C07C251/48

CPC classification number: C07C249/04 ,  C07C249/08 ,  C08K5/33 ,  C09D5/086 ,  C23F11/147 ,  C07C251/48

Abstract: Method for preparation of 5-alkylsalicylaldoximes with formula 1, where R is a C6-C16 alkyl group, consisting in that into a water-alcohol solvent system, p-alkylphenol, sodium hydroxide, chloroform and hydroxylamine are introduced, while in relation to the alkylphenol used, sodium hydroxide and chloroform are used in amounts from the stoichiometric amount to a 100% excess, and hydroxylamine is used in amounts from the stoichiometric amount to a 60% excess, and the reaction is carried out at a temperature of 60-75° C. for 1.5-4 h, and then, at a temperature of 20-30° C., the post-reaction mixture is acidified till the pH of the aqueous phase

公开(公告)号：US10059658B2

公开(公告)日：2018-08-28

申请号：US15694032

申请日：2017-09-01

Applicant: Politechnika Warszawska

Inventor： Krzysztof Bujnowski ,  Ludwik Synoradzki ,  Jerzy Wisialski ,  Agnieszka Krolikowska ,  Jacek Bordzilowski ,  Marcin Koziorowski ,  Roman Zadrozny ,  Anna Jerzak ,  Krzysztof Dzienis

IPC: C07C249/04 ,  C07C249/08 ,  C09D5/08 ,  C23F11/14

CPC classification number: C07C249/04 ,  C07C249/08 ,  C08K5/33 ,  C09D5/086 ,  C23F11/147 ,  C07C251/48

Abstract: Method for preparation of 5-alkylsalicylaldoximes with formula 1, where R is a C6-C16 alkyl group, consisting in that into a water-alcohol solvent system, p-alkylphenol, sodium hydroxide, chloroform and hydroxylamine are introduced, while in relation to the alkylphenol used, sodium hydroxide and chloroform are used in amounts from the stoichiometric amount to a 100% excess, and hydroxylamine is used in amounts from the stoichiometric amount to a 60% excess, and the reaction is carried out at a temperature of 60-75° C. for 1.5-4 h, and then, at a temperature of 20-30° C., the post-reaction mixture is acidified till the pH of the aqueous phase

公开(公告)号：US10011559B2

公开(公告)日：2018-07-03

申请号：US15498726

申请日：2017-04-27

Applicant: SUNOVION PHARMACEUTICALS INC.

Inventor： Hang Zhao ,  Stefan G. Koenig ,  Charles P. Vandenbossche ,  Surendra Singh ,  Harold Scott Wilkinson ,  Roger P. Bakale

IPC: C07C231/14 ,  C07C249/08 ,  C07C209/62 ,  C07C231/12 ,  C07C209/50 ,  C07C211/42 ,  C07B43/06

CPC classification number: C07C231/14 ,  C07B43/06 ,  C07C209/50 ,  C07C209/62 ,  C07C211/42 ,  C07C231/12 ,  C07C249/08 ,  C07C2602/10

Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.

公开(公告)号：US09790223B2

公开(公告)日：2017-10-17

申请号：US15125554

申请日：2015-03-12

Applicant: WOCKHARDT LIMITED

Inventor： Vijay Prakash Chavan ,  Karuna Suresh Wankhede ,  Vikas Vithalrao Deshmukh ,  Satish Bhavsar ,  Kiran Ramchandra Patil ,  Ravindra Dattatraya Yeole ,  Prasad Keshav Deshpande ,  Mahesh Vithalbhai Patel

IPC: C07D471/08 ,  C07F7/18 ,  C07C251/36 ,  C07D211/56 ,  C07C249/08

CPC classification number: C07D471/08 ,  C07C249/08 ,  C07C251/36 ,  C07D211/56 ,  C07F7/1804 ,  C07C251/38

Abstract: A process for preparation of a compound of Formula (I) is disclosed.

公开(公告)号：US09464038B2

公开(公告)日：2016-10-11

申请号：US14892114

申请日：2014-05-20

Applicant: BAYER CROPSCIENCE AKTIENGESELLSCHAFT

Inventor： Albert Schnatterer ,  Dieter Heinz ,  Martin Littmann ,  Ulrich Philipp ,  Juergen Ludwig ,  Constantin Frerick ,  Michael Barz

IPC: C07C249/08 ,  C07F9/09

CPC classification number: C07C249/08 ,  C07F9/09 ,  C07C251/48 ,  C07C251/36 ,  C07C251/44

Abstract: Method for preparing certain oximes and oxime O-methyl ethers by reacting poorly water-soluble carbonyl compounds with salts of hydroxylamine or hydroxylamine O-methyl ether or the free base of hydroxylamine in the presence of certain phosphoric esters or salts thereof of the formula (I) wherein R1, R2 and X are defined as specified in the description.

公开(公告)号：US20160168080A1

公开(公告)日：2016-06-16

申请号：US14436515

申请日：2014-03-26

Applicant: ZCL CHEMICALS LIMITED

Inventor： Nand Lal AGARWAL ,  Trushar Dahyabhai PATEL ,  Pintu Balubhai LORIYA

IPC: C07C249/12 ,  C07C249/08

CPC classification number: C07C249/12 ,  C07C249/08 ,  C07C251/58 ,  C07C251/48

Abstract: The present invention relates to an industrially feasible and economically viable process for the preparation of fluvoxamine maleate of formula I.

Abstract translation: 本发明涉及在工业上可行和经济上可行的制备式I的马氟酸氟伏沙明的方法。

公开(公告)号：US20140364622A1

公开(公告)日：2014-12-11

申请号：US14373439

申请日：2013-02-13

Applicant: Syngenta Participations AG

Inventor： Tomas Smejkal

IPC: C07D231/14 ,  C07C249/08 ,  C07C251/66 ,  C07C45/61 ,  C07C49/573 ,  C07C251/32

CPC classification number: C07D231/14 ,  C07C45/61 ,  C07C49/573 ,  C07C249/08 ,  C07C251/32 ,  C07C251/66

Abstract: The present invention relates to a process for the enantioselective preparation of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxylic acid ((1S,4R)-9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide of formula Ib.

Abstract translation: 本发明涉及对映选择性制备3-二氟甲基-1-甲基-1H-吡唑-4-羧酸（（1S，4R）-9-二氯亚甲基-1,2,3,4-四氢-1 ，4-甲酰基 - 萘-5-基） - 酰胺。

公开(公告)号：US20120296114A1

公开(公告)日：2012-11-22

申请号：US13522465

申请日：2010-12-09

Applicant: Woo Sun Kim

Inventor： Woo Sun Kim

IPC: C07C227/26

CPC classification number: C07C227/04 ,  B01J21/18 ,  B01J23/40 ,  B01J23/44 ,  B01J23/75 ,  C07C249/08 ,  C07C229/38 ,  C07C251/48

Abstract: The present invention relates to a preparation method of 4-aminomethylbenzoic acid comprising the following steps: preparing 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate); reacting the 4-carboxylbenzaldehyde or an alkyl ester thereof (methyl 4-formyl benzoate) with hydroxyamine to oximate the same; and contact reducing 4-carboxylbenzaldehyde oxime or an alkyl ester oxime thereof obtained by the oximation, through hydrogen in a sodium hydroxide aqueous solution. Since methyl 4-hydroxyiminomethylbenzoate is reacted as a raw material in the presence of an alkali, hydrogen of a relatively low pressure can be used and a purification process is also simple, thereby enabling preparation of 4-aminomethylbenzoic acid with a low cost and high yield.

Abstract translation: 本发明涉及4-氨基甲基苯甲酸的制备方法，包括以下步骤：制备4-羧基苯甲醛或其烷基酯（4-甲酰基苯甲酸甲酯）; 使4-羧基苯甲醛或其烷基酯（4-甲酰基苯甲酸酯）与羟胺反应，使其氧化; 并通过氢氧化钠水溶液中的氢气将通过肟化得到的4-羧基苯甲醛肟或其烷基酯肟接触。 由于在碱存在下使4-羟基亚氨基甲基苯甲酸甲酯作为原料反应，所以可以使用相对低压的氢，并且纯化方法也很简单，从而能够以低成本和高产率制备4-氨基甲基苯甲酸 。

公开(公告)号：US08097760B2

公开(公告)日：2012-01-17

申请号：US12281819

申请日：2007-03-30

Applicant: Hang Zhao ,  Stefan G. Koenig ,  Charles P. Vandenbossche ,  Surendra Singh ,  Harold Scott Wilkinson ,  Roger P. Bakale

Inventor： Hang Zhao ,  Stefan G. Koenig ,  Charles P. Vandenbossche ,  Surendra Singh ,  Harold Scott Wilkinson ,  Roger P. Bakale

IPC: C07C321/00 ,  C07C323/00 ,  C07C381/00 ,  C07C211/00

CPC classification number: C07C231/14 ,  C07B43/06 ,  C07C209/50 ,  C07C209/62 ,  C07C211/42 ,  C07C231/12 ,  C07C249/08 ,  C07C2602/10

Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.

Abstract translation: 本发明提供了将肟转化成烯酰胺的方便方法。 该方法不需要使用金属试剂。 因此，它产生所需化合物，而不伴随产生大量的金属废物。 酰胺是酰胺和胺的有用前体。 本发明提供了将前手性烯酰胺转化成相应的手性酰胺的方法。 在示例性方法中，通过使用手性氢化催化剂在氢化期间引入手性氨基中心。 在选择的实施方案中，本发明提供了制备包括1,2,3,4-四氢-N-烷基-1-萘胺或1,2,3,4-四氢-1-萘胺亚结构的酰胺和胺的方法。

公开(公告)号：US07164047B2

公开(公告)日：2007-01-16

申请号：US10493224

申请日：2002-10-31

Applicant: Katsuji Ujita

Inventor： Katsuji Ujita

IPC: C07C29/14 ,  C07C253/30 ,  C07C249/08 ,  C07C255/31

CPC classification number: C07C29/14 ,  C07C45/58 ,  C07C249/08 ,  C07C251/38 ,  C07C253/00 ,  C07C255/31 ,  C07C2601/02 ,  C07C47/11 ,  C07C31/1333

Abstract: A process for preparation of cyclopropylethanol, which comprises subjecting a 3-cyclopropyl-2,3-epoxypropionic acid ester to solvolysis, treating the product of the solvolysis with an acid to obtain cyclopropylacetaldehyde, and reducing the obtained cyclopropylacetaldehyde; and a process for preparation of cyclopropylacetonitrile, which comprises subjecting a 3-cyclopropyl-2,3-epoxypropionic acid ester to solvolysis in the presence of a base, treating the product of the solvolysis with an acid to obtain cyclopropylacetaldehyde, reacting the obtained cyclopropylacetaldehyde with hydroxylamine or salts thereof to obtain cyclopropaneacetaldehyde oxime, and reacting the obtained cyclopropaneacetaldehyde oxime with acetic anhydride. According to the present invention, cyclopropylethanol and cyclopropylacetonitrile can be prepared at low costs and industrially advantageously.

Abstract translation: 一种制备环丙基乙醇的方法，其包括使3-环丙基-2,3-环氧丙酸酯溶解溶剂，用酸处理溶剂分解产物，得到环丙基乙醛，还原所得的环丙基乙醛; 和环丙基乙腈的制备方法，其包括在碱的存在下使3-环丙基-2,3-环氧丙酸酯进行溶剂分解，用酸处理溶剂分解产物，得到环丙基乙醛，将得到的环丙基乙醛与 羟胺或其盐，得到环丙烷乙醛肟，并使得到的环丙烷乙醛肟与乙酸酐反应。 根据本发明，可以低成本且在工业上有利地制备环丙基乙醇和环丙基乙腈。