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91. 发明专利

JPH07196592A NEW ACETIC ACID DERIVATIVE 失效
公开(公告)号：JPH07196592A
公开(公告)日：1995-08-01
申请号：JP30055394
申请日：1994-12-05
申请人： HOFFMANN LA ROCHE
发明人： REO AARITSUHI , POORU HADOBUARII , MARIANNE HIYURUTSUERAA MIYURAA , MARUSERU MIYURAA , BIATO SHIYUTAINAA , TOOMASU BUERAA
IPC分类号： C07D401/12 , A61K31/00 , A61K31/19 , A61K31/22 , A61K31/24 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/395 , A61K31/4418 , A61K31/445 , A61K31/47 , A61K31/472 , A61P7/00 , A61P7/02 , A61P19/00 , C07C237/32 , C07C251/24 , C07C251/48 , C07C257/18 , C07C259/18 , C07C271/06 , C07C271/62 , C07C271/64 , C07C323/42 , C07C323/50 , C07C333/04 , C07D207/12 , C07D211/00 , C07D211/20 , C07D211/34 , C07D211/46 , C07D211/58 , C07D211/94 , C07D213/78 , C07D213/81 , C07D213/82 , C07D217/02 , C07D267/14 , C07D271/06 , C07D271/07 , C07D307/68 , C07D309/12 , C07D413/02 , C07D413/06 , C07D413/10 , C07D413/12 , C07F9/24
摘要： Acetic acid derivatives of the formula in which L, M, Q and T have the meaning stated in the description, can be used for the treatment or prophylaxis of diseases caused by the binding of adhesive proteins to blood platelets, and by aggregation of blood platelets and cell-cell adhesion. They are prepared by eliminating protective groups in corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.

92. 发明专利

JPH07502985A 失效
公开(公告)号：JPH07502985A
公开(公告)日：1995-03-30
申请号：JP50669493
申请日：1992-09-09
IPC分类号： C07D237/10 , A01N47/06 , A01N47/12 , A01N47/16 , A01N47/18 , A01N47/20 , A01N47/22 , C07C68/02 , C07C69/734 , C07C69/96 , C07C249/04 , C07C249/12 , C07C251/38 , C07C251/48 , C07C269/02 , C07C269/04 , C07C271/28 , C07C271/64 , C07C317/42 , C07C323/20 , C07C323/36 , C07C327/48 , C07C329/02 , C07C329/04 , C07C329/14 , C07C333/04 , C07C333/08 , C07D209/08 , C07D213/04 , C07D213/75 , C07D239/28 , C07D241/14 , C07D277/68 , C07D277/70 , C07D277/82 , C07D295/205 , C07D311/76
摘要： Fungicidal compounds having the formula (I): wherein W is CH3O.CH=CCO2CH3, CH3ON=CCONR R or CH3ON=CCO2CH3 and stereoisomers thereof; n is O or 1; X is oxygen or sulphur; Z is oxygen, sulphur or NR ; R is hydrogen or alkyl optionally substituted with halogen, C1-6 alkoxy, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl or aryl; R is alkyl, haloalkyl, alkenyl, alkynyl, alkoxycarbonyl(C1-4)alkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryl(C1-4)alkyl, optionally substituted heteroaryl(C1-4)alkyl, optionally substituted aryloxy(C1-4)alkyl, optionally substituted heteroaryloxy(C1-4)alkyl, optionally substituted aryloxy(C2-4)alkenyl, optionally substituted heteroaryloxy(C2-4)alkenyl, optionally substituted aryl(C2-4)alkenyl, optionally substituted heteroaryl(C2-4)alkenyl, optionally substituted arylcarbonyl(C1-4)alkyl, optionally substituted heteroarylcarbonyl(C1-4)alkyl, optionally substituted aryloxycarbonyl(C1-4)alkyl, optionally substituted heteroaryloxycarbonyl-(C1-4)alkyl or -COR ; or R and R together form an optionally substituted 4-, 5- or 6-membered heterocyclic ring system; R and R are independently hydrogen or methyl; and R is optionally substituted heteroaryl or optionally substituted aryl; and processes for preparing, compositions comprising and methods of combating fungi using compounds of formula (I). Also provided is a process for the preparation of a compound of formula (XX): wherein p is 0 or 1.

93. 发明专利

JPH0466563A PRODUCTION OF UNSATURATED CARBAMATE ESTERS 失效
公开(公告)号：JPH0466563A
公开(公告)日：1992-03-02
申请号：JP17718090
申请日：1990-07-03
申请人： NIPPON PAINT CO LTD
发明人： TSUBONIWA SHIYOUSUKE , YAMANAKA EIJI , URANO SATORU
IPC分类号： C07C269/04 , C07C269/00 , C07C269/06 , C07C271/64
摘要： PURPOSE:To simply obtain the subject compound useful as a monomer for synthesizing polymer materials, etc., in a process by reacting an unsaturated amide compound with a metal base as starting raw materials and subsequently reacting the product with a halogenated formic acid ester. CONSTITUTION:An unsaturated amide compound of formula I (R is H, lower alkyl) is reacted with a metal base such as sodium hydroxide or methyllithium in an inactive solvent (e.g. dioxane or methyl isobutyl ketone) as -20 to 120 deg.C and subsequently reacted with a halogenated formic acid ester of formula II (X is halogen; R is monohydric alcohol residue eliminating hydroxyl group) (e.g. chloroformic acid ethyl ester) at -20 to 100 deg.C, preferably 0 to 50 deg.C, to obtain a compound of formula III. As another method, a compound of formula IV is reacted with the metal base in an inactive solvent and subsequently with a compound of formula V to obtain the compound of formula III.

94. 发明专利

JPH041169A ACYLFORMAMIDE COMPOUND AND PRODUCTION OF FORMAMIDES 失效
公开(公告)号：JPH041169A
公开(公告)日：1992-01-06
申请号：JP10254190
申请日：1990-04-18
申请人： KIKUKAWA YASUO
发明人： KIKUKAWA YASUO
IPC分类号： C07C239/20 , C07C231/04 , C07C259/06 , C07C271/64
摘要： NEW MATERIAL:An acylformamide compound shown by the formula HCO(R CO)N-OR (R is alkyl, aryl, alkoxy or styryl; R is alkyl). EXAMPLE:N-Formylphenethylamine. USE:A formylating agent being readily handleable, stably preservable and inexpensively usable. PREPARATION:An alkoxyamide shown by the formula R CONH-OR is reacted with acetic formic anhydride shown by the formula HCOOCOCH3 in the presence of a base (e.g. pyridine) in a solvent such as methylene chloride to give an acylformamide compound. An amine is selectively formylated with the compound to give a formamide.

95. 发明专利

JPH02300104A BACTERIOCIDAL COMPOSITION FOR AGRICULTURAL AND HORTICULTURAL USE 失效
公开(公告)号：JPH02300104A
公开(公告)日：1990-12-12
申请号：JP10079290
申请日：1990-04-16
申请人： SUMITOMO CHEMICAL CO
发明人： NOGUCHI HIROSHI , KATO TOSHIRO , TAKAHASHI JUNYA , ISHIKURI YUKIO , YAMAMOTO SHIGEO , KAMOSHITA KATSUZO
IPC分类号： A01N47/20 , A01N47/18 , C07C271/28 , C07C271/64 , C07C333/08 , C07C333/10
摘要： PURPOSE:To provide the title composition of great efficacy to chemical-resistant strain, having high blight control effect at low concentration, containing an N-phenylcarbamate compound and a benzimidazole-, thiophanate- or cyclic imide-based bacteriocidal agent. CONSTITUTION:The objective composition containing, as active ingredients, (A) a compound of the formula (R is lower alkyl, lower alkenyl, lower alkynyl, lower haloalkyl, phenyl-substituted lower alkyl, etc.; Y is O or S; Z is H, lower alkylcarbonyl, benzoyl, etc.) and (B) at least one agent selected from benzimidazole-based bacteriocides, thiophanate-based bacteriocides [e.g. methyl 1-(butylcarbamoyl)benzimidazol-2-yl carbamate] and cyclic imide-based bacteriocides. The present composition, when continuously applied on a farm where chemical-resistant strain has not been developed yet, call prevent such bacteria even with concern about the spread thereof.

97. 发明专利

JPH02191216A DRUG FOR FISH PARASITE 失效
公开(公告)号：JPH02191216A
公开(公告)日：1990-07-27
申请号：JP19071289
申请日：1989-07-25
申请人： BAYER AG
发明人： HAINTSU MEERUHORUN , GIYUNTAA SHIYUMAARU , BERUNAA RINDONAA , AKUSERU HAABAAKORUN
IPC分类号： C07D253/06 , A61K31/53 , A61P33/00 , A61P33/02 , C07C271/64 , C07D253/075
摘要： PURPOSE: To obtain a medicine for preventing parasites on fishes, especially parasitic protozoan and metazoa by including a substituted 1,2,4-triazinediones or a salt thereof. CONSTITUTION: This medicine for preventing parasites on fishes includes a compound of the formula [R is an aromatic group or a heterocyclic aromatic group bonded by C; X is O, S, SO, SO2 or C(CN)H; R is H, a halogen, NO2 , an alkyl, an alkoxy, a halogenoalkyl or an halogenoalkoxy; R is H, an alkyl, an alkenyl, an alkynyl or an aralkyl] or a base salt thereof, e.g. 2-chloro-α-(4- chlorophenyl)-4-(4,5-dihydro-3,5-dioxo-1,2,4-triazin-2(3H)-yl)-phenyla cetonitrile. The treatment by the medicine is performed by an addition to a food, a short period treatment by a transcutaneous bath (the concentration is 5-10mg/L) when transferring the fishes between feeding vessels or a temporary or permanent pool treatment (the concentration is 0.1-5mg/L).

98. 发明专利

JPS61137851A Production of carbobenzyloxyacetamidine 失效
标题翻译：生产卡博辛氧乙酰胺
公开(公告)号：JPS61137851A
公开(公告)日：1986-06-25
申请号：JP26042684
申请日：1984-12-10
申请人： Mitsubishi Chem Ind Ltd
发明人： TAMURA MITSUHIKO , YAMADA KENICHI , YABANETA TOSHIHIKO , WASEDA TOSHIE
IPC分类号： C07C271/64 , C07C67/00 , C07C239/00 , C07C269/00
摘要： PURPOSE: To produce a carbobenzyloxyacetamidine, in high selectivity, purity and yield, by reacting a benzyl chloroformate compound with an acetamidine mineral acid salt under specific condition.
CONSTITUTION: The objective compound can be produced by reacting a benzyl chloroformate compound with an acetamidine mineral acid salt. The reaction is carried out at -20W+10°C keeping the pH of the reaction system to ≥11, by using an aqueous solution of the acetamidine mineral acid salt and if necessary an organic solvent such as metylene dichloride, etc., as the base liquid, alkalinizing the liquid to ≥11pH with an aqueous solution of a caustic alkali, and supplying a benzyl chloroformate compound or its organic solvent solution and an aqueous solution of caustic alkali slowly to the mixture. The amounts of the benzyl chloroformate and the caustic alkali are 0.3W1.0mol and 1.3W2.0mol per 1mol of the acetamidine mineral acid salt.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过在特定条件下使氯甲酸苄酯化合物与乙脒无机酸盐反应，以高选择性，纯度和产率制备苄氧羰基乙脒。构成：目标化合物可以通过使氯甲酸苄酯化合物与乙脒无机酸盐反应来制备。反应在-20〜+ 10℃下进行，通过使用乙脒无机酸盐的水溶液，如果需要，可以使用二氯甲烷等有机溶剂，将反应体系的pH值保持在> = 11。作为基础液体，用苛性碱水溶液使液体碱化为> = 11pH，并向混合物缓慢地供给氯甲酸苄酯化合物或其有机溶剂溶液和苛性碱水溶液。氯甲酸苄酯和苛性碱的量为每1mol乙脒无机酸盐为0.3-1.0mol和1.3-2.0mol。

99. 发明专利

JPS608243A ALPHA,ALPHA-DIMETHYLBENZYLHYDROXYLAMINE DERIVATIVE AND HERBICIDE 失效
公开(公告)号：JPS608243A
公开(公告)日：1985-01-17
申请号：JP11594583
申请日：1983-06-29
申请人： SHOWA DENKO KK
发明人： TSURUYA TETSUO , SEKI MINAAKI
IPC分类号： A01N47/24 , A01N37/28 , A01N39/04 , A01N47/28 , A01N47/30 , C07C67/00 , C07C239/00 , C07C259/04 , C07C259/10 , C07C271/12 , C07C271/64 , C07C275/64 , C07C301/00 , C07C311/48 , C07C325/00 , C07C335/40
摘要： NEW MATERIAL:The alpha,alpha-dimethylbenzylhydroxylamine derivative of formula I [Y is H, lower alkyl, lower alkylcarbamoyl, or phenylcarbamoyl; Z is group of formula II (X is O or S; R is alkyl, methyl phenyl aralkyl, or phenoxymethyl; R' is H or methyl), -C(=O), -C(=O)OR or group of formula III]. EXAMPLE:The compound of formula I wherein Y is H and Z is group of formula IV. USE:Herbicide having strong herbicidal activity to a wide range of weeds, and effective by the application to the weeds immediately before sprouting or at the initial stage of growth. It kills the weeds in the field of paddy rice plant, corn, potato, soybean, wheat, orchard, etc. PREPARATION:The compound of formula VI which is one of the compound of formula I can be prepared by reacting the compound of formula V (novel compound) with the compound of formula R-N=C=X in a solvent such as benzene, toluene, etc. The starting compound of formula V is obtained by the half-reduction of alpha-nitrocumene.

100. 发明专利

JPS59212460A N-substituted amidine derivative and production thereof 失效
标题翻译： N-取代的氨基衍生物及其生产方法
公开(公告)号：JPS59212460A
公开(公告)日：1984-12-01
申请号：JP8785083
申请日：1983-05-19
申请人： Sankyo Co Ltd
发明人： OKADA YASUSHI , HASHIMOTO MITSUNORI , YOSHIHARA HISAYOSHI , TAKEBAYASHI TOYONORI , EDA YUTAKA , OSANAI YASUTOMO
IPC分类号： C07D207/12 , C07C67/00 , C07C239/00 , C07C257/10 , C07C257/12 , C07C257/14 , C07C257/18 , C07C257/20 , C07C269/00 , C07C271/64 , C07D213/75 , C07D227/12 , C07D247/00 , C07D249/02 , C07D253/00 , C07C123/00 , C07C125/063
摘要： NEW MATERIAL:A compound of formula I [R
1 is H, (halogen-substituted) lower alkyl or phenyl which may have a substituent group (a lower alkoxyl, halogen or nitro, etc.) etc.; R
2 is aralkyloxycarbonyl, allyloxycarbonyl or aralkyl, etc.].
EXAMPLE: N-(p-Nitrobenzyloxycarbonyl)formamidine.
USE: Useful as a synthetic intermediate for penem and carbapenem derivatives having improved antimicrobial activity.
PREPARATION: A compound of formula II or a salt thereof is reacted with a compound of the formula R
2 -X
1 (X
1 is azido) in an organic solvent at room temperatureW-70°C, preferably room temperature W-15°C to give the compound of formula I . The reaction is carried out using equimolar amounts of the compound of formula II and the compound of the formula R
2 -X
1 . Alternatively, the compound of formula II is reacted with a compound of the formula R
2 -X
2 (X
2 is halogen) in the presence of a base to afford the compound of formula I .
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I化合物[R 1]为H，（卤素取代的）低级烷基或可具有取代基的苯基（低级烷氧基，卤素或硝基等）等; R 2是芳烷氧基羰基，烯丙氧羰基或芳烷基等]。实施例：N-（对硝基苄氧羰）甲脒。用途：作为具有改善的抗微生物活性的青枯烯和碳青霉烯衍生物的合成中间体。制备：将式II化合物或其盐与式R 2 -X 1的化合物（X 1为叠氮基）在有机溶剂中在室温-70℃反应，优选室温-15℃，得到式I化合物。反应使用等摩尔量的式II化合物和式R 2 -X 1的化合物进行。或者，式II化合物与式R 2 -X 2的化合物（X 2是卤素）在碱的存在下反应，得到式I化合物。

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