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公开(公告)号:JP2001294551A
公开(公告)日:2001-10-23
申请号:JP2001021329
申请日:2001-01-30
Applicant: BAYER AG
Inventor: MARHOLD ALBRECHT , STOELTING JOERN
Abstract: PROBLEM TO BE SOLVED: To provide a method for producing a 3,5-bis(trifluoromethyl)benzoyl chloride from a readily available starting material, surely practicable on an industrial scale, and to obtain intermediate(s) formed during the above process. SOLUTION: This method comprises the following steps: a 3,5-dimethylbenzoic acid is converted to the corresponding acid chloride, which, in turn, is completely chlorinated in a free radical fashion at the side chains to form the corresponding 3,5-bis(trichloromethyl)benzoyl chloride, which is then fluorinated with anhydrous hydrogen fluoride and/or antimony pentafluoride to produce the corresponding 3,5-bis(trifluoromethyl)benzoyl fluoride, which, in turn, is reacted in the presence of silicon tetrachloride and an additional Lewis acid to obtain the objective compound of the general formula I (X is H, F or Cl). By the way, some of the 3,5-bis(trihalogenomethyl)- and 3,5-dimethylbenzoyl compounds as intermediates are new compounds.
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公开(公告)号:JP2001081065A
公开(公告)日:2001-03-27
申请号:JP2000241124
申请日:2000-08-09
Applicant: BAYER AG
Inventor: MARHOLD ALBRECHT , STOELTING JOERN
Abstract: PROBLEM TO BE SOLVED: To provide a process for the production of subject compounds from an easily available starting material without necessitating the handling of highly toxic carcinogenic substances. SOLUTION: [Bis-(trifluoromethyl)-phenyl]-acetic acids are produced by reacting a proper bromo- or iodo-bis-(trifluoromethyl)-benzene with a di-(1-4C)- alkyl malonate in the presence of a deprotonation agent and a copper salt and hydrolyzing and decarboxylating the product in a basic medium. The reaction mixture before the hydrolysis and complete decarboxylation is mixed with water and an acid and heated and distilled under reduced pressure to separate an alkyl [bis-(trifluoromethyl)-phenyl]-acetate and a dialkyl [bis-(trifluoromethyl)- phenyl]-malonate is obtained by column chromatography, etc.
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公开(公告)号:WO9954326A8
公开(公告)日:1999-12-29
申请号:PCT/EP9902344
申请日:1999-04-07
Applicant: BAYER AG , STOLTEFUSS JUERGEN , GOLDMANN SIEGFRIED , KRAEMER THOMAS , SCHLEMMER KARL HEINZ , NIEWOEHNER ULRICH , PAESSENS ARNOLD , GRAEF ERWIN , LOTTMANN STEFAN , DERES KARL , WEBER OLAF , STOELTING JOERN
Inventor: STOLTEFUSS JUERGEN , GOLDMANN SIEGFRIED , KRAEMER THOMAS , SCHLEMMER KARL-HEINZ , NIEWOEHNER ULRICH , PAESSENS ARNOLD , GRAEF ERWIN , LOTTMANN STEFAN , DERES KARL , WEBER OLAF , STOELTING JOERN
IPC: C07D213/78 , A61K31/506 , A61P1/16 , A61P31/12 , C07D213/00 , C07D213/84 , C07D215/00 , C07D239/00 , C07D239/22 , C07D277/62 , C07D401/04 , C07D401/14 , C07D417/14
CPC classification number: C07D239/22 , C07D213/78 , C07D213/84 , C07D401/04 , C07D401/14
Abstract: The invention relates to compounds of general formula (I) or general formula (Ia). The invention also relates to methods for producing said compounds of general formula (I) or (Ia) and to their use as medicaments, especially for treating and preventing hepatitis B.
Abstract translation: 本发明涉及通式(I)或(Ia)的化合物。 本发明还涉及用于制备式(I)或(Ia)和它们作为药物的用途,特别是对肝炎B的治疗和预防的化合物
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公开(公告)号:BR0116727A
公开(公告)日:2003-12-23
申请号:BR0116727
申请日:2001-12-28
Applicant: BAYER AG
Inventor: SEIDEL ANDREAS , BAUMANN KAETHE , ECKEL THOMAS , ZOBEL MICHAEL , STOELTING JOERN , WITTMANN DIETER
Abstract: An oligophosphate of general formula is disclosed. The oligophosphate is suitable as a flame retardant for thermoplastic molding compositions that exhibit a good flame-retardant effect, improved dimensional stability under the effect of heat, a good level of toughness and excellent flowability.
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公开(公告)号:DE10121652A1
公开(公告)日:2002-11-07
申请号:DE10121652
申请日:2001-05-03
Applicant: BAYER AG
Inventor: STOELTING JOERN , VAN LAAK KAI , SIRGES WOLFRAM
IPC: C07D277/20 , C07D213/61 , C07D277/32 , C07D307/14 , C07D417/12 , C07D213/53 , C07D405/06
Abstract: The invention relates to a method for producing compounds of formula (I) by reacting compounds of formula (II), in which R , R , R and Het each have the meanings as cited in the description, with anhydrous hydrogen halide while in the presence of a nitrile.
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公开(公告)号:PL341973A1
公开(公告)日:2001-02-26
申请号:PL34197300
申请日:2000-08-11
Applicant: BAYER AG
Inventor: MARHOLD ALBRECHT , STOELTING JOERN
Abstract: Preparation of (bis-(trifluoromethyl)-phenyl)-acetic acids (I) involves (a) reacting a bromo- or iodo-bis-(trifluoromethyl)-benzene (II) with a di-(1-4C alkyl) malonate (III) in presence of a deprotonating reagent and a copper salt, then (b) saponifying and decarboxylating the product in a basic medium. Also new are a method for preparing dialkyl phenylmalonates (IV) and alkyl phenylacetates (V) using step (a); and the compounds (IV). Independent claims are included for: (i) the preparation of (bis-(trifluoromethyl)-phenyl)-acetic acid esters, by step (a) as above followed by cooling the reaction mixture, acidifying to pH 5-9, separating the solids, washing the residue with an ether or alcohol and recovering product from the combined filtrate and washings by distillation under reduced pressure; (ii) the preparation of a mixture of dialkyl phenylmalonates of formula (IV) and alkyl phenylacetates of formula (V), by step (a) as above followed (before saponification and complete decarboxylation) by treating the reaction mixture with water and acid, heating and working up the mixture by extraction and distillation; (iii) the preparation of (IV) by working up the mixture obtained in (ii) by column chromatography, fractional distillation or thin film distillation; (iv) the preparation of (V) by working up the mixture obtained in (ii) by distillation under reduced pressure; and (v) (IV) as new compounds. R = 1-4C alkyl.
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公开(公告)号:BR9910896A
公开(公告)日:2001-02-13
申请号:BR9910896
申请日:1999-05-21
Applicant: BAYER AG
Inventor: ALIG BERND , MARHOLD ALBRECHT , STOELTING JOERN , GAU WOLFGANG , ERDELEN CHRISTOPH , TURBERG ANDREAS , MENCKE NORBERT , HANSEN OLAF
IPC: A01N43/56 , C07D231/44 , C07D401/04
Abstract: The invention relates to novel substituted 3-thiocarbamoylpyrazoles of general formula (I), wherein m, n, R1, R2, R3 and Ar have the meanings cited in the description. The invention further relates to methods for the production and use thereof as pesticides.
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公开(公告)号:TR200003011T2
公开(公告)日:2001-01-22
申请号:TR200003011
申请日:1999-04-07
Applicant: BAYER AG
Inventor: STOLTEFUSS JUERGEN , GOLDMANN SIEGFRIED , KRAMER THOMAS , SCHLEMMER KARL-HEINZ , NIEWOEHNER ULRICH , PAESSENS ARNOLD , GRAEF ERWIN , LOTTMANN STEFAN , DERES KARK , WEBER OLAF , STOELTING JOERN
IPC: A61K31/506 , A61P1/16 , A61P31/12 , C07D213/78 , C07D213/00 , C07D213/84 , C07D215/00 , C07D239/00 , C07D239/22 , C07D277/62 , C07D401/04 , C07D401/14 , C07D417/14
Abstract: The invention relates to compounds of the formule
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公开(公告)号:CZ293482B6
公开(公告)日:2004-05-12
申请号:CZ20003871
申请日:1999-04-07
Applicant: BAYER AG
Inventor: STOLTEFUSS JUERGEN , GOLDMANN SIEGFRIED , KRAEMER THOMAS , SCHLEMMER KARL-HEINZ , NIEWOEHNER ULRICH , PAESSENS ARNOLD , GRAEF ERWIN , LOTTMANN STEFAN , DERES KARL , WEBER OLAF , STOELTING JOERN
IPC: C07D213/78 , A61K31/506 , A61P1/16 , A61P31/12 , C07D213/00 , C07D213/84 , C07D215/00 , C07D239/00 , C07D239/22 , C07D277/62 , C07D401/04 , C07D401/14 , C07D417/14
Abstract: The present invention relates to dihydropyrimidine compounds of the general formula I, optionally Ia, in which the substituents have specific meanings, process of their preparation, intermediates for their preparation, as well as their use for preparing medicaments suitable for treating and prophylaxis of viral diseases, in particular hepatitis B.
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公开(公告)号:DE59902573D1
公开(公告)日:2002-10-10
申请号:DE59902573
申请日:1999-04-07
Applicant: BAYER AG
Inventor: STOELTING JOERN , STOLTEFUSS JUERGEN , GOLDMANN SIEGFRIED , KRAEMER THOMAS , SCHLEMMER KARL-HEINZ , NIEWOEHNER ULRICH , PAESSENS ARNOLD , GRAEF ERWIN , LOTTMANN STEFAN , DERES KARL , WEBER OLAF
IPC: C07D213/78 , A61K31/506 , A61P1/16 , A61P31/12 , C07D213/00 , C07D213/84 , C07D215/00 , C07D239/00 , C07D239/22 , C07D277/62 , C07D401/04 , C07D401/14 , C07D417/14
Abstract: The invention relates to compounds of the formule
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