公开(公告)号：EP4430025A1

公开(公告)日：2024-09-18

申请号：EP21963602.4

申请日：2021-11-11

Applicant: ADAMA MAKHTESHIM LTD.

Inventor： GRABARNICK, Michael ,  WU, Shaoxiang ,  GAO, Rui ,  WANG, Rui ,  WANG, Wenjun ,  LIU, Wei

IPC: C07C251/24

CPC classification number: C07C251/24 ,  C07C249/02 ,  C07C201/10 ,  C07C213/02 ,  C07D333/38 ,  C07F3/02

公开(公告)号：EP3256444A1

公开(公告)日：2017-12-20

申请号：EP16704711.7

申请日：2016-02-11

Applicant: Novartis AG

Inventor： MARTIN, Benjamin ,  MANDRELLI, Francesca ,  VENTURONI, Francesco

IPC: C07C201/12 ,  C07C227/04 ,  C07C335/16

CPC classification number: C07C201/10 ,  B01J31/0237 ,  B01J31/0241 ,  B01J31/0244 ,  B01J31/0265 ,  C07B2200/07 ,  C07C201/12 ,  C07C205/04 ,  C07C205/44 ,  C07C205/51 ,  C07C227/04 ,  C07C335/16 ,  C07C2601/14 ,  C07C2602/08 ,  C07D207/06 ,  C07F7/1804 ,  C07F9/5355 ,  C07C205/53 ,  C07C229/34

Abstract: The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.

公开(公告)号：EP2247568A1

公开(公告)日：2010-11-10

申请号：EP09716009.7

申请日：2009-02-26

Applicant: Bromine Compounds Ltd.

Inventor： OREN, Jacob

IPC: C07C201/12 ,  C07C205/15

CPC classification number: C07C201/10 ,  C07C201/12 ,  C07C205/15

Abstract: The invention provides a process for preparing bronopol, which process comprises charging a reaction vessel with water, bromopicrin, nitromethane and paraformaldehyde, gradually feeding a base into said reaction vessel under stirring, bringing the reaction to completion and separating bronopol from the aqueous reaction mixture.

公开(公告)号：EP2206697A1

公开(公告)日：2010-07-14

申请号：EP10001844.9

申请日：2006-01-12

Applicant: Schering Corporation

Inventor： Wu, George G. ,  Sudhakar, Anantha ,  Wang, Tao ,  Xie, Ji ,  Chen, Frank Xing ,  Poirier, Marc ,  Huang, Mingsheng ,  Sabesen, Vijay ,  Kwok, Daw-long ,  Cui, Jian ,  Yang, Xiaojing ,  Thiruvengadam, Tiruvettipuram K. ,  Liao, Jing

IPC: C07C205/55 ,  C07C205/44 ,  C07C309/08

CPC classification number: C07D263/56 ,  C07C69/606 ,  C07C69/732 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C205/55 ,  C07C231/10 ,  C07C231/12 ,  C07C235/28 ,  C07C303/32 ,  C07C309/08 ,  C07C2601/16 ,  C07D277/64 ,  C07D307/92 ,  C07D333/56 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  C07F7/1852 ,  C07F9/582 ,  Y02P20/55 ,  C07C233/28

Abstract: This application discloses compounds which are useful in the preparation of himbacine analogs as well as processes for their preparation:

Abstract translation: 本申请公开了可用于制备烟肼类似物的化合物及其制备方法：

公开(公告)号：EP1077955A1

公开(公告)日：2001-02-28

申请号：EP99922160.9

申请日：1999-05-04

Applicant: BASF AKTIENGESELLSCHAFT

Inventor： RHEINHEIMER, Joachim ,  VON DEYN, Wolfgang ,  GEBHARDT, Joachim ,  RACK, Michael ,  LOCHTMAN, Rene ,  GÖTZ, Norbert ,  KEIL, Michael ,  WITSCHEL, Matthias ,  HAGEN, Helmut ,  MISSLITZ, Ulf ,  BAUMANN, Ernst

IPC: C07D261/04 ,  C07D413/10 ,  C07C251/40 ,  C07C319/14

CPC classification number: C07C249/06 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C209/62 ,  C07C251/48 ,  C07C253/00 ,  C07C255/50 ,  C07C315/04 ,  C07C319/14 ,  C07D261/04 ,  C07D413/10 ,  C07C323/09 ,  C07C317/24 ,  C07C317/32 ,  C07C205/06 ,  C07C211/52

Abstract: The invention relates to a method for producing isoxazolene of the formula (I), where the substituents have the following meanings: R1 is hydrogen, C¿1?-C6 alkyl, R?2 is C¿1-C6 alkyl, R?3, R4, R5¿ are hydrogen, C¿1?-C6 alkyl or R?4 and R5¿ together form a linkage, R6 is a heterocyclic ring, and n is 0, 1 or 2. Said method comprises the production of an intermediate compound of the formula (VI) where R?1, R3, R4 and R5¿ have the meanings given above. This step is followed by halogenation, thiomethylation, oxidation and acylation to yield compounds of formula (I). The invention also relates to new intermediate products for producing compounds of formula (I) and new methods for producing the intermediate products.

公开(公告)号：EP1021412A1

公开(公告)日：2000-07-26

申请号：EP96941744.3

申请日：1996-12-09

Applicant: The Secretary of State for Defence

Inventor： MILLAR, Ross, Wood ,  CLARIDGE, Robert, Peter ,  SANDALL, John, Paul, Benet ,  THOMPSON, Claire

IPC: C07D213/76 ,  C07D213/61 ,  C07D241/16 ,  C07D241/20 ,  C07D239/42 ,  C07D239/30 ,  C07D251/42 ,  C07D251/26 ,  C07C381/10 ,  C07C205/12 ,  C07B43/02

CPC classification number: C07D213/76 ,  C07C201/10 ,  C07C201/16 ,  C07C381/10 ,  C07D213/61 ,  C07D239/42 ,  C07D241/16 ,  C07D241/20 ,  C07D251/44 ,  C07D251/46 ,  C07C205/12 ,  C07C205/06

Abstract: A method of nitrating electron-deficient carbocyclic or heterocyclic aromatic compounds such as pyridines, diazines and triazines and benzenoid aromatics having electron-withdrawing substituents involves first reacting the aromatic species with a sulphilimine species or with the corresponding N-alkali metal salt thereof to generate an N-(hetero)aryl-S,S-dialkyl, diaryl or alkylarylsulphilimine derivative. This intermediate may then be readily oxidised under relatively mild conditions using a peroxycarboxylic acid such as m-chloroperbenzoic acid, peracetic or peroxytrifluoroacetic acid. Good yields of nitrated products are obtained including some previously unprepared. The novel N-alkali(alkylaryl)sulphilimine reagents are prepared by reacting an alkali metal hydride, an alkali metal hydrogenous base or an alkyl lithium with the corresponding sulphilimine. Preferred salts are the N-lithio types and the preferred sulphilimine is diphenylsulphilimine. Where the salt is used reaction should be in an aprotic solvent but if the sulphilimine per se is the reagent a polar solvent is used.

公开(公告)号：EP2298749B1

公开(公告)日：2014-12-24

申请号：EP10177806.6

申请日：1999-05-04

Applicant: BASF SE

Inventor： Rheinheimer, Joachim ,  von Deyn, Wolfgang ,  Gebhardt, Joachim ,  Rack, Michael ,  Lochtman, Rene ,  Götz, Norbert ,  Keil, Michael ,  Witschel, Matthias ,  Hagen, Helmut ,  Mißlitz, Ulf ,  Baumann, Ernst

IPC: C07D261/04 ,  C07D413/10 ,  C07C251/40 ,  C07C319/14

CPC classification number: C07C249/06 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C209/62 ,  C07C251/48 ,  C07C253/00 ,  C07C255/50 ,  C07C315/04 ,  C07C319/14 ,  C07D261/04 ,  C07D413/10 ,  C07C323/09 ,  C07C317/24 ,  C07C317/32 ,  C07C205/06 ,  C07C211/52

公开(公告)号：EP2196468A1

公开(公告)日：2010-06-16

申请号：EP10001846.4

申请日：2006-01-12

Applicant: Schering Corporation

Inventor： Wu, George G. ,  Sudhakar, Anantha ,  Wang, Tao ,  Xie, Ji ,  Chen, Frank Xing ,  Poirier, Marc ,  Huang, Mingsheng ,  Sabesen, Vijay ,  Kwok, Daw-long ,  Cui, Jian ,  Yang, Xiaojing ,  Thiruvengadam, Tiruvettipuram K. ,  Liao, Jing

IPC: C07F9/58

CPC classification number: C07D263/56 ,  C07C69/606 ,  C07C69/732 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C205/55 ,  C07C231/10 ,  C07C231/12 ,  C07C235/28 ,  C07C303/32 ,  C07C309/08 ,  C07C2601/16 ,  C07D277/64 ,  C07D307/92 ,  C07D333/56 ,  C07D405/06 ,  C07D413/06 ,  C07D417/06 ,  C07F7/1852 ,  C07F9/582 ,  Y02P20/55 ,  C07C233/28

Abstract: This application discloses a compound which is useful in the preparation of himbacine analogs as well as processes for its preparation:

wherein R 9 is selected from the group consisting of C 1 -C 10 alkyl, aryl, heteroaryl, and arylalkyl.

Abstract translation: 本申请公开了一种可用于制备烟肼类似物的化合物及其制备方法：其中R 9选自C 1 -C 10烷基，芳基，杂芳基和芳基烷基。

公开(公告)号：EP1077955B1

公开(公告)日：2007-06-27

申请号：EP99922160.9

申请日：1999-05-04

Applicant: BASF Aktiengesellschaft

Inventor： RHEINHEIMER, Joachim ,  VON DEYN, Wolfgang ,  GEBHARDT, Joachim ,  RACK, Michael ,  LOCHTMAN, Rene ,  GÖTZ, Norbert ,  KEIL, Michael ,  WITSCHEL, Matthias ,  HAGEN, Helmut ,  MISSLITZ, Ulf ,  BAUMANN, Ernst

IPC: C07D261/04 ,  C07D413/10 ,  C07C251/40 ,  C07C319/14

CPC classification number: C07C249/06 ,  C07C201/10 ,  C07C201/12 ,  C07C205/44 ,  C07C209/62 ,  C07C251/48 ,  C07C253/00 ,  C07C255/50 ,  C07C315/04 ,  C07C319/14 ,  C07D261/04 ,  C07D413/10 ,  C07C323/09 ,  C07C317/24 ,  C07C317/32 ,  C07C205/06 ,  C07C211/52

Abstract: The invention relates to a method for producing isoxazolene of the formula (I), where the substituents have the following meanings: R1 is hydrogen, C¿1?-C6 alkyl, R?2 is C¿1-C6 alkyl, R?3, R4, R5¿ are hydrogen, C¿1?-C6 alkyl or R?4 and R5¿ together form a linkage, R6 is a heterocyclic ring, and n is 0, 1 or 2. Said method comprises the production of an intermediate compound of the formula (VI) where R?1, R3, R4 and R5¿ have the meanings given above. This step is followed by halogenation, thiomethylation, oxidation and acylation to yield compounds of formula (I). The invention also relates to new intermediate products for producing compounds of formula (I) and new methods for producing the intermediate products.

公开(公告)号：EP1486479A1

公开(公告)日：2004-12-15

申请号：EP04253380.2

申请日：2004-06-07

Applicant: MITSUI CHEMICALS, INC.

Inventor： Funaki, Setsuko, c/o Mitsui Chemicals, Inc. ,  Taniguchi, Yoshiteru, c/o Mitsui Chemicals, Inc. ,  Nobori, Tadahito, c/o Mitsui Chemicals, Inc. ,  Yamamoto, Yoshihiro, c/o Mitsui Chemicals, Inc. ,  Hara, Isao, c/o Mitsui Chemicals, Inc. ,  Hayashi, Takaomi, c/o Mitsui Chemicals, Inc. ,  Mizutani, Kazumi, c/o Mitsui Chemicals, Inc. ,  Kiyono, Shinji, c/o Mitsui Chemicals, Inc.

IPC: C07B39/00 ,  C07B37/04 ,  C07B41/00 ,  C07B43/00 ,  C07D307/24 ,  C07D307/14 ,  C07C17/20 ,  C07C253/14 ,  C07C255/19 ,  C07C331/18 ,  C07D307/32 ,  C07C319/14 ,  C07C45/63 ,  C07C205/02 ,  C07C209/08 ,  C07F9/06

CPC classification number: C07D307/33 ,  C07B37/04 ,  C07B41/00 ,  C07B43/00 ,  C07C17/208 ,  C07C29/124 ,  C07C67/10 ,  C07C67/11 ,  C07C67/287 ,  C07C201/10 ,  C07C209/08 ,  C07C253/14 ,  C07C253/30 ,  C07C319/14 ,  C07C331/14 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2603/18 ,  C07D307/14 ,  C07D307/24 ,  C07C23/08 ,  C07C69/003 ,  C07C323/22 ,  C07C205/02 ,  C07C323/56 ,  C07C255/46 ,  C07C255/41 ,  C07C255/20 ,  C07C255/19 ,  C07C255/16 ,  C07C255/03 ,  C07C211/42 ,  C07C69/145 ,  C07C69/24 ,  C07C69/63 ,  C07C33/24

Abstract: The invention pertains to a method in which a halogen atom of an organic compound is replaced with a group derived from a nucleophilic agent, at high yield and high efficiency, by the following method which includes a step of reacting the nucleophilic agent with an organic material having a halogen atom bonded to a carbon atom having four σ bonds, more specifically: a method for producing an organic compound having Q, the method including a step of reacting a compound represented by general formula (2) with an organic starting material having at least one halogen atom bonded to a carbon atom having four σ bonds so as to replace the halogen atom in the organic starting material with Q:

        MQ a      (2)

(wherein M represents an alkali metal atom, an alkali earth metal atom, or a rare earth metal atom; Q represents a moiety of an inorganic acid or an active hydrogen compound derived by eliminating a proton, wherein Q is a halogen atom different from the halogen atom in the organic starting material having the halogen atom bonded to the carbon atom having the four σ bonds; and a represents an integer of 1 to 3) in the presence of a compound represented by general formula (1)
(wherein Z - represents an anion derived by eliminating a proton from an inorganic acid or an active hydrogen compound; R 2 is the same or different; R 2 each independently represent a C 1 -C 10 hydrocarbon group or two R 2 on the same nitrogen atom may be bonded with each other to form a ring with the nitrogen atom).

Abstract translation: 本发明涉及一种方法，其中有机化合物的卤素原子以高产率和高效率被来自亲核剂的基团替代，包括使亲核剂与有机材料反应的步骤 具有与具有四个σ键的碳原子键合的卤素原子，更具体地说：一种制备具有Q的有机化合物的方法，所述方法包括使通式（2）表示的化合物与具有式 与具有四个σ键的碳原子键合的至少一个卤素原子，以用Q：MQa（其中M表示碱金属原子，碱土金属原子或稀土金属原子）代替有机原料中的卤素原子 ; Q表示无机酸或通过除去质子衍生的活性氢化合物的部分，其中Q是与有机起始垫中的卤素原子不同的卤素原子 具有与具有四个σ键的碳原子键合的卤素原子的化合物; （1）表示的化合物（其中Z 1表示通过从无机酸或活性氢化合物中除去质子而得到的阴离子）的存在下，a表示1〜3的整数。 R2相同或不同; R2各自独立地表示C1-C10烃基，或者相同氮原子上的两个R2可以彼此键合以与氮原子形成环）。