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81. 发明专利

JPS62103092A BETA-LACTAM DERIVATIVE 失效
公开(公告)号：JPS62103092A
公开(公告)日：1987-05-13
申请号：JP16667886
申请日：1986-07-17
申请人： SAGAMI CHEM RES
发明人： TSUNEMOTO DAIEI , KOBORI TAKEO
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:The compound of formula I R and R are H or amino- protecting group; R is H, salt-forming cation, protecting group of carboxylic acid or anion; R is H or CH2R (R is H or residue of nucleophilic compound); X is S or >N-Me]. EXAMPLE:(Z)-7-(2-aminothiazol-4-yl)-2-{[5-amino-1,2,4-thiadiazol-3-yl) methoxyimi no]acetamido}-3-acetoxymethyl-3-cephem-4-carboxyl ic acid sodium salt. USE:An antibacterial agent having excellent antibacterial activity against Gram- positive bacteria, Gram-negative bacteria, Pseudomonas aeruginosa, myxomycetes and Escherichia coli. PREPARATION:The compound of formula II is made to react with the compound of formula III or its salt and, if necessary, the amino-protecting group is eliminated from the product.

82. 发明专利

JPS60116663A N-PROPARGYL-N-(2-TRIFLUOROMETHYLBENZOYL)-3-SUBSTITUTED BENZENESULFONAMIDE AND SELECTIVE HERBICIDE CONTAINING SAID COMPOUND AS ACTIVE COMPONENT 失效
公开(公告)号：JPS60116663A
公开(公告)日：1985-06-24
申请号：JP22442883
申请日：1983-11-30
申请人： SAGAMI CHEM RES , CENTRAL GLASS CO LTD
发明人： TSUNEMOTO DAIEI , SAKAI HIDEKO , KONDOU SEI , HAYASHI KAORU , WATANABE MASAHIRO , KOMATA TAKEO , MOTOJIMA KENJI
IPC分类号： A01N41/06 , C07C67/00 , C07C301/00 , C07C311/51
摘要： NEW MATERIAL:The compound formula I (R is halogen, lower alkyl, nitro, cyano, etc.; R is H, halogen, lower alkoxy, etc.). EXAMPLE:N-propargyl-3-chlorobensenesulfonamide. USE:Herbicide for paddy rice field, grain field, orchard, lawn, pasture land, tea plantation, mulberry plantation, rubber plantation, etc. PREPARATION:The compound of formula I can be produced by reacting the benzenesulfonyl chloride derivative of formula II with propargylamine of formula III, and reacting the resultant N-propargylbenzenesulfonamide derivative of formula IV with 2-trifluoromethylbenzoyl halide of formula V. The reaction can be carried out smoothly in the presence of a base (e.g. NaOH), preferably in a solvent (e.g. acetone) at a temperature between 0 deg.C and the refluxing temperature of the solvent.

83. 发明专利

JPS603309B2 失效
公开(公告)号：JPS603309B2
公开(公告)日：1985-01-26
申请号：JP14610577
申请日：1977-12-07
申请人： SAGAMI CHEM RES
发明人： KONDO SEI , TSUNEMOTO DAIEI , KISHI KUMIKO
IPC分类号： C07D333/12 , C07D333/16 , C07D333/22 , C07D333/24 , C07D333/28

84. 发明专利

JPS5935371B2 JPS5935371B2 - 失效
公开(公告)号：JPS5935371B2
公开(公告)日：1984-08-28
申请号：JP13936578
申请日：1978-11-14
申请人： Sagami Chem Res
发明人： KONDO SEI , FUJIMOTO TAMOTSU , SUDA MINORU , TSUNEMOTO DAIEI
IPC分类号： C07D333/24 , C07B31/00 , C07B41/08 , C07C51/00 , C07C51/093 , C07C57/00 , C07C57/30 , C07C57/32 , C07C57/58 , C07C59/00 , C07C59/64 , C07C67/00 , C07C313/00 , C07C323/56 , C07D207/337 , C07D307/54

85. 发明专利

JPS5935370B2 JPS5935370B2 - 失效
公开(公告)号：JPS5935370B2
公开(公告)日：1984-08-28
申请号：JP13936478
申请日：1978-11-14
申请人： Sagami Chem Res
发明人： KONDO SEI , FUJIMOTO TAMOTSU , SUDA MINORU , TSUNEMOTO DAIEI
IPC分类号： C07D333/24 , C07B31/00 , C07B41/08 , C07C51/00 , C07C51/093 , C07C57/00 , C07C57/30 , C07C57/32 , C07C57/58 , C07C59/00 , C07C59/64 , C07C67/00 , C07C313/00 , C07C323/56 , C07D207/337 , C07D307/54 , C07D317/16 , C07D317/60

86. 发明专利

JPS5846513B2 失效
公开(公告)号：JPS5846513B2
公开(公告)日：1983-10-17
申请号：JP922779
申请日：1979-01-31
申请人： SAGAMI CHEM RES
发明人： KONDO SEI , NEGISHI AKIRA , TSUNEMOTO DAIEI
IPC分类号： C07D207/32 , C07D207/333

87. 发明专利

JPS58164593A BETA-LACTAM COMPOUND 失效
公开(公告)号：JPS58164593A
公开(公告)日：1983-09-29
申请号：JP4559382
申请日：1982-03-24
申请人： SAGAMI CHEM RES
发明人： TSUNEMOTO DAIEI , KOBORI TAKEO , KONDOU SEI , MURAKAMI YASUO , TOSHIOKA KICHI , SAKUMA OSAMU , KOJIMA ETSUKO
IPC分类号： C07D501/20 , A61K31/545 , A61K31/546 , A61P31/04
摘要： NEW MATERIAL:A compound (salt) of formulaI R1 is (substituted)thiazolyl (mercapto) or (substituted)phenyl; R2 is halogen, cyano, carbamoyl, lower alkylmercapto or O-lower alkylcarboxyimidoyl; R3 is H, salt-forming cation or protecting group of the carboxylic acid . EXAMPLE:7- 2-Chloromethylene-2-(2-aminothiazol-4-yl)actamido -3-(2-methyl-1, 3, 4-thiadiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid. USE:An antimicrobial agent against Gram-positive, Gram-negative bacteria, Pseudomonas aeruginosa, myxomycetes, coliform bacilli etc. capable of exhibiting a particularly powerful antimicrobial activity even against resistant Gram- negative bacteria. PROCESS:A compound of formula II or a reactive derivative (salt) at the amino group is reacted with an acid of formula III or a reactive derivative (salt) at the COOH group thereof.

88. 发明专利

JPS57146756A PREPARATION OF 2-FORMYL-6-PHENOXYPYRIDINE 失效
公开(公告)号：JPS57146756A
公开(公告)日：1982-09-10
申请号：JP3249381
申请日：1981-03-09
申请人： SAGAMI CHEM RES
发明人： TSUNEMOTO DAIEI , KONDOU SEI , SAITOU AKEMI
IPC分类号： C07D213/64
摘要： PURPOSE:To obtain the titled compound useful as an intermediate for preparing an agricultural chemical in high yield, by reacting 2-methyl-6-phenoxypyridine obtained from a 2-halo-6-methylpyridine with a phenol as a raw material with a halogenating reagent, followed by hydrolyzing it. CONSTITUTION:2-Methyl-6-phenoxypyridine is reacted with a halogenating agent such as chlorine or bromine to give a 2-dihalomethyl-6-phenoxypyridine, which is hydrolyzed under a basic condition with preferably an alkali metal acetate or alkaline earth metal acetate to give 2-formly-6-phenoxypyridine.

89. 发明专利

JPS5767581A Beta-lactam derivative 失效
标题翻译： BETA-LACTAM衍生物
公开(公告)号：JPS5767581A
公开(公告)日：1982-04-24
申请号：JP13299480
申请日：1980-09-26
申请人： Sagami Chem Res Center
发明人： TSUNEMOTO DAIEI , KOBORI TAKEO , KOUNO HIROMICHI , KONDOU SEI
IPC分类号： C07D499/44 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D499/46 , C07D501/26 , C07D501/34 , C07D501/36
CPC分类号： Y02P20/55
摘要： NEW MATERIAL:The β-lactam derivative of formulaI[R
1 is aromatic group residue; Z is group of formula II or formula III (R
2 is H, salt-forming cation, or carboxylic acid protecting group; R
3 is H or residue of nucleophilic compound); X
1 and X
2 are H or halogen, provided that X
1 and X
2 are not H at the same time].
EXAMPLE: 7-(2-Dichloromethylene-2-phenylacetamido)-3-acetoxymethyl-3-cephem-4- carboxylic acid.
USE: An antibacterial agent having broad antibacterial spectrum, effective not only to Gram-positive bacteria but also to Gram-negative bacteria, esp. Pseudomonas aeruginosa, Myxomycetes, and colon bacilli, and having strong antibacterial activity against resistant Gram-negative bacteria.
PROCESS: The compound of formulaIis prepared by reacting the compound of formula IV, its reactive derivative at the amino group, or their salts with the acid of formula V, its reactive derivative at the carboxyl group, or their salts.
COPYRIGHT: (C)1982,JPO&Japio
摘要翻译：新材料：式Ⅰ的β-内酰胺衍生物[R 1]为芳族残基; Z是式II或式III的基团（R 2是H，成盐阳离子或羧酸保护基; R 3是H或亲核化合物的残基）; X 1和X 2均为H或卤素，条件是X 1和X 2不同时为H。实施例7-（2-二氯亚甲基-2-苯基乙酰胺基）-3-乙酰氧基甲基-3-头孢烯-4-羧酸。用途：具有广谱抗菌谱的抗菌剂，不仅对革兰氏阳性菌有效，而且对革兰阴性菌也有效铜绿假单胞菌，粘液菌和大肠杆菌，对抗革兰氏阴性菌具有很强的抗菌活性。方法：式I的化合物是通过式IV化合物，其在氨基上的反应性衍生物或其盐与式V的酸，其在羧基上的反应性衍生物或其盐反应而制备的。

90. 发明专利

JPS5649354A PRODUCTION OF 22AROYLFORMYL SUBSTITUTED PYRROLE DERIVATIVE 失效
公开(公告)号：JPS5649354A
公开(公告)日：1981-05-02
申请号：JP12415679
申请日：1979-09-28
申请人： SAGAMI CHEM RES
发明人： KONDOU SEI , NEGISHI AKIRA , TSUNEMOTO DAIEI
IPC分类号： C07D207/333
摘要： PURPOSE:The formylation of a readily available 2-aroylpyrrole derivative is conducted by the use of an adduct of a formamide derivative and thionyl chloride or oxalyl chloride to produce the titled compound used as a synthetic intermediate of an anti- inflammatory in high yield. CONSTITUTION:An adduct from a formamide derivative such as dimethylformamide or N-formylmorpholine and at least one selected from the group consisting of thionyl chloride and oxalyl chloride, i.e., a Vilsmeyer reagent, is made to react with a 2-aroylpyrrole derivative of formula I (R is H, alkyl, aryl; X is alkyl, alkyloxy, halogen) such as 1-methyl-2-p-methylbenzoylpyrrole, preferably at -20-60 deg.C to form the objective compound of formula II such as 1-methyl-2-formyl-5-p-methylbenzoylpyrrole.

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