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公开(公告)号：JPH0830063B2
公开(公告)日：1996-03-27
申请号：JP3217887
申请日：1987-02-14
发明人： YOSHIDA CHOSAKU , INABA TAKIHIRO , TANAKA KEIICHI , TAKENO TAKATSUNE , NAGAKI HIDEYOSHI , OOTA KENJI , SHIMOTORI TOMOYA , MAKINO SHINJI , TAKANO SHUNTARO
IPC分类号： C07D233/58 , A61K31/415 , A61P25/04 , A61P29/00 , C07D233/64 , C07D405/06
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公开(公告)号：JPH07267943A
公开(公告)日：1995-10-17
申请号：JP249295
申请日：1995-01-11
发明人： TAKANO SHUNTARO , YOSHIDA CHOSAKU , INABA TAKIHIRO , TANAKA KEIICHI , TAKENO TAKATSUNE , NAGAKI HIDEYOSHI , SHIMOTORI TOMOYA , MAKINO SHINJI
IPC分类号： C07D311/22 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/41 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P25/04 , A61P29/00 , A61P37/08 , C07D311/24 , C07D311/32 , C07D311/36 , C07D311/38 , C07D311/42 , C07D405/12 , C07D407/12 , C07D409/12
摘要： PURPOSE:To provide a new 2,3-dihydro-4H-1-benzopyran-4-one derivative useful as an intermediate for a 4H-1-benzopyran-4-one derivative having excellent anti-inflammatory action, antipyretic analgesic action, antiarthritic action and antiallergic action. CONSTITUTION:This benzopyranone derivative is expressed by formula I [R1 is a (halogen-substituted)lower alkyl, a lower alkenyl or an aryl; R is H, an alkyl or an acyl; R is H, a halogen, cyano, a (substituted)alkyl, etc.; R is H, a halogen, NO2, cyano, carboxyl, etc.; R is a (substituted)phenyl, thionyl, a furyl, etc.; Z is O, S or imino] or its salt, e.g. 2,3-dihydro-7- methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one. The compound of formula I is produced by cyclizing a compound of formula II (R is R ; R is R ) with a condensing agent such as phosphorus pentoxide.
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公开(公告)号：JPH0527638B2
公开(公告)日：1993-04-21
申请号：JP6222684
申请日：1984-03-31
发明人： IMAIZUMI HIROYUKI , INABA TAKIHIRO , TAKENO TAKATSUNE , MORITA SEIJI , MUROTANI YOSHIHARU , YOSHIDA JUNICHI , TAKASHIMA KENICHI , TAKANO SHUNTARO , SAIKAWA ISAMU
IPC分类号： C07D501/46 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/56
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4.发明专利
公开(公告)号：JPH0597840A
公开(公告)日：1993-04-20
申请号：JP29206791
申请日：1991-10-11
IPC分类号： A61K31/35 , A61K31/352 , A61K31/353 , A61P29/00 , C07D311/22
摘要： PURPOSE:To produce the subject compound useful as an antiinflammatory agent on an industrial scale in high yield with short steps by reacting a specific benzene derivative with a nitrile derivative or its salt and cyclizing the obtained compound. CONSTITUTION:The objective 3-acylamino-6-phenyloxy-7-alkylsulfonylamino-4H-1- benzopyran-4-one of formula 4 (e.g. 3-acetylamino-7-methylsulfonylamino-6- phenoxy-4H-1-benzopyran-4-one) can be produced by reacting a benzene derivative of formula 1 (R is phenyl which may be substituted with halogen; R is lower alkyl; R is H or lower alkyl) with a nitrile derivative of formula 2 (R is H or acyl which may be substituted with halogen) (e.g. aminoacetonitrile) or its salt to get a compound of formula 3 or its salt and cyclizing the obtained compound.
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公开(公告)号：JPH0375545B2
公开(公告)日：1991-12-02
申请号：JP10310982
申请日：1982-06-17
发明人： SADAKI HIROSHI , IMAIZUMI HIROYUKI , TAKEDA KENJI , INABA TAKIHIRO , TAKENO TAKATSUNE , MORITA SEIJI , KAJITA TETSUYA , SAIKAWA ISAMU
IPC分类号： C07D277/20 , C07C45/63 , C07C45/79 , C07C45/82 , C07D277/38 , C07D277/40 , C07D277/46 , C07D277/48
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公开(公告)号：JPH024227B2
公开(公告)日：1990-01-26
申请号：JP5452284
申请日：1984-03-23
发明人： IMAIZUMI HIROYUKI , INABA TAKIHIRO , TAKENO TAKATSUNE , MORITA SEIJI , MUROTANI YOSHIHARU , YOSHIDA JUNICHI , TAKASHIMA KENICHI , TAKANO SHUNTARO , SAIKAWA ISAMU
IPC分类号： C07D501/04 , C07D501/20 , C07D501/46
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公开(公告)号：JPS63239274A
公开(公告)日：1988-10-05
申请号：JP3217887
申请日：1987-02-14
发明人： YOSHIDA CHOSAKU , INABA TAKIHIRO , TANAKA KEIICHI , TAKENO TAKATSUNE , NAGAKI HIDEYOSHI , OTA KENJI , SHIMOTORI TOMOYA , MAKINO SHINJI , TAKANO SHUNTARO
IPC分类号： C07D233/58 , A61K31/415 , A61P25/04 , A61P29/00 , C07D233/64 , C07D405/06
摘要： NEW MATERIAL:A compound expressed by formula I (R and R are phenyl or heterocyclic group; R is H, alkyl or cycloalkyl; R is H, CN, alkyl, cycloalkyl, aryl or heterocyclic group; R and R are H, halogen, CN, NO2, acyl, alkoxy, aryloxy, alkylthio, alkyl, aryl, etc.; R and R together with C to which they are linked may form 5--7-membered cycloalkenyl ring; R and R together with C to which they are linked may form 3--8-membered cycloalkyl ring) and salt thereof. EXAMPLE:2-[(E)-2-Cyano-1-phenylvinyl]-4,5-bis(4-methoxyphenyl)-1H-imid azole. USE:An anti-inflammatory agent, antipyretic, analgesic agent and antiarthritic agent. PREPARATION:For example, a compound expressed by formula II (R is R except CN) is subjected to the Wittig reaction to afford the corresponding compound expressed by formula I.
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公开(公告)号：JPS6267089A
公开(公告)日：1987-03-26
申请号：JP20623285
申请日：1985-09-20
发明人： IMAIZUMI HIROYUKI , INABA TAKIO , YOSHIDA JUNICHI , YOSHINO OSAMU , TAKENO TAKATSUNE , TAKANO SHUNTARO , SAIKAWA ISAMU
IPC分类号： C07D501/12 , C07D501/46
摘要： PURPOSE:To purify the titled compound useful as an antibacterial agent in high yield and purity easily on an industrial scale, by treating cephalosporin with dioxane and eliminating dioxane from the resultant dioxane adduct. CONSTITUTION:The cephalosporin of formula I (syn isomer) is treated with dioxane to obtain a dioxane adduct of formula II (syn isomer). The adduct is separated and dioxane is eliminated therefrom to obtain the cephalosporin of formula I (syn isomer) s a purified product.
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公开(公告)号：JPH07206869A
公开(公告)日：1995-08-08
申请号：JP30282094
申请日：1994-11-11
发明人： IMAIZUMI HIROYUKI , INABA TAKIHIRO , YOSHIDA JUNICHI , YOSHINO OSAMU , TAKENO TAKATSUNE , TAKANO SHUNTARO , SAIKAWA ISAMU
IPC分类号： C07D319/12 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/46
摘要： PURPOSE:To obtain a new compound, useful as a synthetic intermediate for cephem compounds which are excellent antimicrobial agents and capable of industrially providing the cephem compounds in high yield and purity. CONSTITUTION:This dioxane addition compound of 7beta-[(Z)-2-(2-aminothiazol-4- yl)-2-methoxyiminoacetamido]-3-[(5-methyl-2H-tetrazol-2-yl)methyl]-DEL TA -cephem-4- carboxylic acid (syn-isomer) is expressed by formula I. The compound is obtained by acylating a compound (syn-isomer) expressed by formula 11 (X is a halogen) or its salt with a compound expressed by formula III or its salt in a solvent such as THF usually at -35 to +25 deg.C for several min to several hr, providing a compound expressed by formula IV (syn-isomer) or its salt, then dehydrating the resultant compound and subsequently treating the dehydrated compound with dioxane under acidic conditions of preferably pH2.5-3.
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10.发明专利
公开(公告)号：JPH0249778A
公开(公告)日：1990-02-20
申请号：JP25081188
申请日：1988-10-06
发明人： TAKANO SHUNTARO , YOSHIDA CHOSAKU , INABA TAKIHIRO , TANAKA KEIICHI , TAKENO TAKATSUNE , NAGAKI HIDEYOSHI , SHIMOTORI TOMOYA , MAKINO SHINJI
IPC分类号： C07D213/70 , A61K31/34 , A61K31/35 , A61K31/352 , A61K31/38 , A61K31/40 , A61K31/4025 , A61K31/41 , A61K31/425 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/443 , A61K31/4433 , A61K31/445 , A61P29/00 , C07C311/08 , C07D20060101 , C07D213/62 , C07D213/74 , C07D257/04 , C07D295/12 , C07D295/18 , C07D311/22 , C07D311/24 , C07D311/26 , C07D311/30 , C07D311/36 , C07D311/42 , C07D311/54 , C07D311/56 , C07D311/58 , C07D333/30 , C07D405/00 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D409/14 , C07D417/04
摘要： NEW MATERIAL:The compound of formula I (R is alkyl, alkenyl or aryl; R is H, alkyl or acryl; R is H, halogen, cyano, azido, carboxyl, OH, alkyl, phenyl, etc.; R is H, halogen, nitro, cyano, acyl, OH, alkyl, alkoxy, etc.; R is phenyl, thienyl, furyl or pyridyl; Z is O, S or NH) and its salt. EXAMPLE:6-(2-Fluorophenoxy)-3-formylamino-7-methylsulfonylamino-4H--1- benzopyran-4-one. USE:An anti-inflammatory agent having excellent anti-inflammatory action, antipyretic and analgesic action, anti-arthritic action and anti-allergic action and scarcely exhibiting ulcer-inducing action. PREPARATION:The compound of formula I can be produced e.g., by cyclizing a compound of formula III induced from a compound of formula II and, as necessary, dehydrogenating the cyclized product.
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