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C07C45/57：··氧作为惟一的杂原子

序号	专利名	申请号	申请日	公开（公告）号	公开（公告）日	发明人
161	METHOD FOR PRODUCING CYCLIC DIKETONE COMPOUND	EP23779739.4	2023-03-17	EP4501896A1	2025-02-05	KASHIWAGI Yuki; DEGUCHI Jun
Provided is a method for producing a compound represented by General Formula (I) through oxidative cleavage of a compound of Formula (II), which is a bicyclic tetrasubstituted olefin compound. This method is for producing a compound represented by General Formula (I), including a step of obtaining a compound represented by General Formula (I) through oxidative cleavage of a compound represented by General Formula (II) using an oxidant in the presence of an additive represented by General Formula (III). The definitions of Formula -A^1- and Formula -A^2- in Formulas (I) and (II) above and R, R¹, R², R³, R⁴, and R⁵ in Formula (III) above are as described in the specification.
162	AN EFFICIENT PROCESS FOR THE SYNTHESIS OF ALKOXY SUBSTITUTED BENZALDEHYDES	EP15728614.7	2015-04-29	EP3237394A1	2017-11-01	MOHAPATRA, Manoj Kumar; BENDAPUDI, Ramamohanrao; MENACHERRY, Paul Vincent; PAUL, Vincent
The present invention relates to the synthesis of alkoxy substituted benzaldehydes obtained from the corresponding alkoxy substituted benzenes. Alkoxy substituted benzaldehydes are products of broad commercial interest and are used as end products and intermediates in flavor and fragrance applications and pharmaceutical ingredients. For example, 3,4-methylendioxybenzaldehyde (also known as heliotropin or piperonal) is used widely both as a end product and intermediate for the above mentioned applications. Other examples include 3,4-dimethoxybenzaldehyde, 3,4,5- trimethoxybenzaldehyde and 3,4-ethylenedioxybenzene which are intermediates in the synthesis of active pharmaceutical intermediates.
163	NOVEL BETA-HYDROXYKETONES AND BETA-ALKOXYKETONES WITH ESTROGENIC ACTIVITY	EP08851712.3	2008-11-21	EP2227449A1	2010-09-15	Pulkkinen, Juha; Honkakoski, Paavo; Peräkylä, Mikael; Berczi, Istvan; Laatikainen, Reino
This invention relates to β-hydroxyketones and β-alkoxyketones of formula (I), to their use as estrogen receptor modulators, and to methods for their preparation.
164	Fluorhaltige Benzaldehyde	EP03026982.3	2003-11-26	EP1428814A1	2004-06-16	Peilstöcker, Karen, Dr.; Marhold, Albrecht, Dr.
Die vorliegende Erfindung betrifft fluorhaltige Benzaldehyde, ein Verfahren zu deren Herstellung sowie die Anwendung der fluorhaltigen Benzaldehyde zur Herstellung von Wirkstoffen insbesondere in Arzneimitteln und Agrochemikalien.
165	Production methods of alpha, alpha, alpha-trifluoromethylphenyl-substituted benzoic acid and intermediate therefor	EP01102094.8	2001-01-31	EP1122234A9	2002-01-16	Shintaku, Tetsuya, c/o Sumika Fine Chem. Co., Ltd.; Tanaka, Masahide, c/o Sumika Fine Chem. Co., Ltd.; Shiratani, Hiroshi, c/oSumika Fine Chem. Co., Ltd.; Itaya, Nobushige, c/o Sumika Fine Chem. Co., Ltd.
The present invention relates to a production method of compound [V] useful as an intermediate for medicaments and agrochemicals. The method includes reacting compound [III] with hexamethylenetetramine under heating to give compound [IV], and oxidizing the obtained compound [IV] with a halous acid salt or a ruthenium compound. According to the present invention, moreover, an organometallic compound having a tolyl group and compound [I] are cross-coupled in the presence of a catalyst to give compound [II] useful as an intermediate for medicaments and agrochemicals. The compound [II] is halogenated to give compound [III]. wherein X is halogen atom.
166	Production methods of alpha, alpha, alpha-trifluoromethylphenyl-substituted benzoic acid and intermediate therefor	EP01102094.8	2001-01-31	EP1122234A3	2001-09-12	Shintaku, Tetsuya, c/o Sumika Fine Chem. Co., Ltd.; Tanaka, Masahide, c/o Sumika Fine Chem. Co., Ltd.; Shiratani, Hiroshi, c/oSumika Fine Chem. Co., Ltd.; Itaya, Nobushige, c/o Sumika Fine Chem. Co., Ltd.
The present invention relates to a production method of compound [V] useful as an intermediate for medicaments and agrochemicals. The method includes reacting compound [III] with hexamethylenetetramine under heating to give compound [IV], and oxidizing the obtained compound [IV] with a halous acid salt or a ruthenium compound. According to the present invention, moreover, an organometallic compound having a tolyl group and compound [I] are cross-coupled in the presence of a catalyst to give compound [II] useful as an intermediate for medicaments and agrochemicals. The compound [II] is halogenated to give compound [III]. wherein X is halogen atom.
167	Production methods of alpha, alpha, alpha-trifluoromethylphenyl-substituted benzoic acid and intermediate therefor	EP01102094.8	2001-01-31	EP1122234A2	2001-08-08	Shintaku, Tetsuya, c/o Sumika Fine Chem. Co., Ltd.; Tanaka, Masahide, c/o Sumika Fine Chem. Co., Ltd.; Shiratani, Hiroshi, c/oSumika Fine Chem. Co., Ltd.; Itaya, Nobushige, c/o Sumika Fine Chem. Co., Ltd.
The present invention relates to a production method of compound [V] useful as an intermediate for medicaments and agrochemicals. The method includes reacting compound [III] with hexamethylenetetramine under heating to give compound [IV], and oxidizing the obtained compound [IV] with a halous acid salt or a ruthenium compound. According to the present invention, moreover, an organometallic compound having a tolyl group and compound [I] are cross-coupled in the presence of a catalyst to give compound [II] useful as an intermediate for medicaments and agrochemicals. The compound [II] is halogenated to give compound [III]. wherein X is halogen atom.
168	PROCEDE DE FONCTIONNALISATION D'UN COMPOSE PHENOLIQUE PORTEUR D'UN GROUPE ELECTRO-DONNEUR	EP98947631.2	1998-10-08	EP1027326A1	2000-08-16	MIOKOWSKI, Charles; WAGNER, Alain; BENSEL, Nicolas; PEVERE, Virginie; DESMURS, Jean-Roger
The invention concerns a method for functionalizing a phenolic compound bearing an electron-donor group, in said group para position, inter alia a method for the amidoalkylation of a phenolic compound bearing an electron-donor group, and more particularly a phenolic compound bearing an electron-donor group preferably, in the hydroxyl group ortho position. The method for functionalizing in para position with respect to an electron-donor group carried by a phenolic compound is characterised in that the phenolic compound bearing an electron-donor group is subjected to the following steps: a first step which consists in protecting the hydroxyl group in the form of a sulphonic ester function; a second step which consists in reacting the protected phenolic compound with an electrophilic reagent; optionally a third step deprotecting the hydroxyl group.
169	HYDROXYCYCLOPENTANONE	EP98923077.6	1998-06-01	EP0990635A1	2000-04-05	KOJIMA, Kaoru Biomedical Group; IKAI, Katsushige Central Research Laboratories; ENOKI, Tatsuji Central Research Laboratories; KOYAMA, Nobuto Central Research Laboratories; KATO, Ikunoshin Central Research Laboratories
2,3,4-trihydroxycyclopentanone represented by the following formula [I], its optically active substance or salt thereof.
170	VERFAHREN ZUR HERSTELLUNG VON N-BUTYRALDEHYD UND/ODER N-BUTANOL	EP95930520.2	1995-08-24	EP0778819B1	1999-01-13	KANAND, Jürgen; RÖPER, Michael; PACIELLO, Rocco; THOME, Alfred

171	FORMYLATION PROCESS FOR AROMATIC ALDEHYDES	EP94906619.5	1994-01-26	EP0690835B1	1998-08-19	GODEK, Dennis, M.; SNYDER, William, M.; STEWART, Andrew, M.
A novel two-step reaction process for preparing 5-substituted-2-methoxybenzaldehyde compounds is disclosed wherein the substituent group is either isopropyl or trifluoromethoxy. The process involves (1) reacting a corresponding 4-substituted phenol compound with dimethyl carbonate in the presence of a tertiary-amine base to form the corresponding 4-substituted anisole compound, and (2) thereafter subjecting the latter intermediate product obtained in the first step to aromatic C-formylation on the ring with hexamethylenetetramine in the presence of trifluoroacetic acid, followed by hydrolysis, to ultimately yield the desired aldehyde compound. The two aromatic aldehyde compounds so obtained, viz., 2-methoxy-5-trifluoromethoxybenzaldehyde and 2-methoxy-5-isopropylbenzaldehyde, are known to be useful as intermediates that specifically lead to (2S^_,3S^_)-c^_i^_s^_-3-(2-methoxy-5-trifluoromethoxybenzyl)amino-2-phenylpiperidine and (2S^_,3S^_)-c^_i^_s^_-2-(diphenylmethyl)-N-[(2-methoxy-5-isopropylphenyl)methyl]-1-azabicyclo[2.2.2.]octane-3-amine, respectively. The latter final products, in turn, are both known to be useful in the field of medicinal chemistry as substance P receptor antagonists.
172	Process for 3,5-di-tert-butylsalicylaldehyde	EP94307744.6	1994-10-21	EP0650952A1	1995-05-03	Gao, Yun; Nie, Xiaoyi
A process for the synthesis of 3-5-tert-butyl-salicylaldehyde from 2,4-di-tert-butylphenol and hexamethylenetetramine is disclosed. The reaction provides 3,5-tert-butylsalicylaldehyde in commercially attractive yields from readily available starting materials.
173	Procédé de transformation de N-oxydes d'amines tertiaires en aldéhydes	EP91401508.6	1991-06-10	EP0461972A1	1991-12-18	Chabardes, Pierre; Henrot, Serge; Mercier, Claude
L'invention concerne un procédé de transformation de N-oxydes d'amines tertiaires en aldéhydes au moyen d'un catalyseur dérivé du vanadium, ainsi que la préparation d'aldéhydes insaturés à partir de diènes.
174	Process for the preparation of beta-hydroxyketones	EP90103939.6	1990-03-01	EP0387612A3	1991-03-13	Lin, You-Jyh; Kloczewski, Harold
A process for the preparation of β-hydroxyketones comprising the catalytic hydrogenolysis of an aqueous solution of isoxazolines having the formula in a fixed bed reactor containing a transition metal catalyst at a temperature between 20 to 150°C and a pressure from about 0 to 150 psig; wherein R₁ and R₂ are independently selected from hydrogen, alkyl, cycloalkyl or aromatic group and wherein the aqueous solution of isoxazolines is substantially free of acids or buffers.
175	NEUE RIECHSTOFFE	EP82900537.0	1982-02-25	EP0073771B1	1985-09-18	BAUDIN, Josiane; GONZENBACH, Hans Ulrich
New odoriferous compounds, particularly the compounds having the following formula: <IMAGE> wherein R is an aliphatic residue having the formula <IMAGE> wherein R<1> is a C1-4 alkyl, C1-4 alkylidene or C2-4 alkenyl, the sum of the carbon atoms being in those residues from 2 to 5, m and n being equal to zero or 1, p being 1, 2 or 3 and the dotted lines representing one or two optional double bonds. The invention also relates to a method for the preparation of new di-ketones I; as well as the use of I as odoriferous compounds in odoriferous compositions, which are characterized by a certain proportion of compounds having the formula I.
176	Conversion of hexafluorothioacetone dimer into hexafluoroacetone	EP82102345.4	1982-03-22	EP0066678B1	1985-06-05	Anello, Louis Gene

177	Keto-aldehyde derivatives and process for their preparation	EP83105896	1983-06-16	EP0097882A3	1984-05-16	Ditgens, Klaus, Dr.; Krämer, Wolfgang, Dr.; Elbe, Hans-Ludwig, Dr.
Die Erfindung betrifft neue Keto-aldehyd-Derivate, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Zwischenprodukte zur Synthese von Azolyl-ketonen und -alkoholen, welche fungizide und pflanzenwachstumsregu lierende Eigenschaften besitzen. Die Verbindungen der Formel in welcher R¹ und R² die in der Beschreibung angegebene Bedeu tung besitzen, können erhalten werden, wenn man Säurechloride mit 1-(N-Morpholino)-isobuten in Gegenwart eines Verdün nungsmittels umsetzt und hydrolysiert, sowie gegebenen falls die so erhaltenen Ketoaldehyde in üblicher Weise an der Aldehydgruppe derivatisiert. Die Verbindungen können zB durch Umsetzung mit Azolen, wie 1,2,4-Triazol, und anschließender Alkylierung in Azolyl-ketone und -alkohole mit fungizider und das Pflanzen wachstum regulierender Wirkung überführt werden.
178	Optically active or racemic aminal derivatives, process for preparing same and for converting same to alpha-hydroxyaldehydes	EP79302419.1	1979-11-02	EP0011417B1	1983-05-04	Mukaiyama, Teruaki; Sakito, Yoji; Asami, Masatoshi

179	Conversion of hexafluorothioacetone dimer into hexafluoroacetone	EP82102345.4	1982-03-22	EP0066678A1	1982-12-15	Anello, Louis Gene
The production of hexafluoroacetone by contacting, in the liquid phase, hexafluorothioacetone dimer with at least a stoichiometric amount of an aprotic solvent selected from the group consisting of dimethylacetamide, dimethylformamide, dimethyl sulfoxide and N-methyl pyrrolidone and at least a catalytic amount of an alkali metal fluoride or a sulfonic acid having general formula RSO,H ist disclosed. Dimethylformamide and dimethyl sulfoxide are the preferred aprotic solvents; KF is the preferred alkali metal fluoride; and CH₃SO₃H and pCH₃C₆H₄SO₃H are the preferred sulfonic acids. The production of hexafluoroacetone by contacting hexafluoropropene with elemental sulfur and a catalytic amount of an alkali metal fluoride in an aprotic solvent at a temperature of between about 40 and about 70 °C for a time sufficient to produce hexafluorothioacetone dimer combined with increasing the temperature to between about 90 and 150°C and maintaining said temperature for a time sufficient to produce hexafluoroacetone is also disclosed.
180	Optically active or racemic alpha-hydroxyaldehydes and benzyl derivatives thereof	EP81108506.7	1979-11-02	EP0050351A1	1982-04-28	Mukaiyama, Teruaki; Sakito, Yoji; Asami, Masatoshi
An optically active or racemic a-hydroxyaldehyde of formula and a compound having a benzyloxy group in place of its hydroxy group, wherein R, represents a C₆-C₁₄ aryl group, C₁-C₁₀alkyl group, C₃-C₁₀ alkenyl group, C₂-C₁₀ alkynyl group, C₇-C₁₄ aralkyl group, or a group containing a functional group in the organic portion of said groups, and R₂ represents a C₁-C₁₀ alkyl group, C₁-C₁₀ alkenyl group, C₂-C₁₀ alkynyl group, C₇-C₁₄ aralkyl group, C₆-C₁₄ aryl group or a group containing a functional group in the organic portion of these groups, R, and R₂ being different groups, is an important intermediate for preparation of pharmaceuticals and agricultural chemicals.

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