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91. 发明专利

JP2000198774A OPTICALLY ACTIVE GUANIDINE DERIVATIVE 失效
公开(公告)号：JP2000198774A
公开(公告)日：2000-07-18
申请号：JP197099
申请日：1999-01-07
申请人： SHIRATORI PHARM
发明人： ISOBE TOSHIO , FUKUDA KEIKO
IPC分类号： C07D233/48 , B01J31/02 , C07D301/19 , C07D303/32
摘要： PROBLEM TO BE SOLVED: To obtain a new compound useful as an asymmetric synthesis reagent capable of selectively producing an optically active compound in high yield. SOLUTION: This new compound is a compound of formula I (R1 and R2 are each an alkyl; R3 is an (OH-contg.) aralkyl or heterocyclic ring; *, denotes an asymmetric carbon atom), e.g. 1,3-bis[(1S)-1-phenylethyl]-2-[(1S)-1- phenylethylimino]imidazolidine. The compound of formula I is obtained, for example, by reaction between a compound of formula II (Z is a halogen) e.g. 2-chloro-1,3-bis[(1S)-1-phenylethyl]imidazolinium chloride) and a primary amine of the formula H2N-R3 [e.g. (S)-α-phenethylamine] in the presence of a base such as triethylamine, wherein it is preferable that either the compound of formula II or the above primary amine is previously dissolved in a solvent such as methylene chloride and the other is gradually dripped into the resulting solution at room temperature or under cooling.

92. 发明专利

JPH11158074A AMINO ACID-RICH ACTIVE VITAMIN D POTENTIATION COMPOSITION 失效
公开(公告)号：JPH11158074A
公开(公告)日：1999-06-15
申请号：JP33254797
申请日：1997-12-03
申请人： HAYASHI TOMIE , SHIRATORI PHARM
发明人： HAYASHI HIROMICHI
IPC分类号： A23L1/30 , A23L33/10 , A23L33/155 , A61K31/59 , A61K35/22 , A61K35/407 , A61K35/57 , A61K35/60 , A61K36/18 , A61K36/185 , A61K36/54 , A61P3/02 , A23L1/303 , A61K35/23 , A61K35/78
摘要： PROBLEM TO BE SOLVED: To obtain an active vitamin D potentiation composition permitting to efficiently absorb active vitamins D. SOLUTION: This amino acid-rich active vitamin D potentiation composition is obtained by adding the homogenate of liver and kidney of domestic fowls or fishes and the powdered geranium herb or powdered cinnamon bark to vitamin D2 and/or vitamin D3 followed by stirring at 25-40 deg.C.

93. 发明专利

JPH10236971A ACTIVATED VITAMIN D ENRICHED COMPOSITION ADDED WITH HIGH AMINO ACID COMPONENT 失效
公开(公告)号：JPH10236971A
公开(公告)日：1998-09-08
申请号：JP33254897
申请日：1997-12-03
申请人： HAYASHI TOMIE , SHIRATORI PHARM
发明人： HAYASHI HIROMICHI
IPC分类号： A23L1/30 , A23L1/305 , A23L33/10 , A23L33/135 , A23L33/155 , A23L33/17 , A61K31/195 , A61K31/59 , A61K35/22 , A61K35/407 , A61K35/57 , A61K35/60 , A61K36/07 , A61P3/02 , A61K35/84 , A23L1/303 , A61K35/23
摘要： PROBLEM TO BE SOLVED: To obtain the subject composition capable of allowing a person to effectively ingest vitamin D by adding the homogenate of liver and kidney of poultry and fishes to a pulverized material of mushrooms, and stirring the pulverized material with the added homogenate at a specific temperature. SOLUTION: The objective composition is obtained by adding the homogenate of liver and kidney of poultry and fishes to a pulverized material of mushrooms (preferably Auricularia auricula), and stirring the pulverized material with the added homogenate at 25-40 deg.C, preferably 37 deg.C. Preferably, the mushrooms are pulverized to 10-100μm by a pulverizer, irradiated by ultraviolet rays of 295nm by a high-pressure mercury-vapor lamp for 10sec to 1min while shaking and stirring the pulverized mushroom, thereafter heated at 90-110 deg.C for 30min to 1hr, air-cooled and mixed with the homogenates. A freshwater eel is preferable as the poultry and the fishes. A mixing weight ratio of the mushrooms to the homogenates is preferably (1:1) to (1:5). When the homogenates are added, 5-10wt.% powder of Cinnamomi Cortex based on the weight of the mushrooms is preferably added thereto. Further, the stirring time is preferably 30-60min.

94. 发明专利

JPH10195051A PRODUCTION OF AZASPIRO(4,5)DECATRIENONES 失效
公开(公告)号：JPH10195051A
公开(公告)日：1998-07-28
申请号：JP436597
申请日：1997-01-14
申请人： SHIRATORI PHARM
发明人： ISOBE TOSHIO
IPC分类号： C07D209/54 , B01J31/02 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To obtain the subject compound in a short time in high yield by reacting an oxime as a raw material by using a specific haloiminium salt in the vicinity of neutrality under a mild condition. SOLUTION: An oxime of a formula I (R is hydroxy or an alkoxy; R is an alkyl) is reacted with about 1mol of a haloiminium, salt of formula II (R and R are each a lower alkyl; X is a halogen; (n) is 2 or 3) such as 2-chloro-1,3- dimethylimidazolium chloride by adding about 2mols of a base such as 2,6- lutidine at about a room temperature to give azaspiro[4,5]decatrienones of formula III. After the reaction is over, the compounds are isolated by a conventional method such as distillation or recrystallization.

95. 发明专利

JPH08239787A PRODUCTION OF 4-FLUORO-2-AZETIDINONE DERIVATIVE 失效
公开(公告)号：JPH08239787A
公开(公告)日：1996-09-17
申请号：JP4271595
申请日：1995-03-02
申请人： SHIRATORI PHARM
发明人： SUDA KOJI
IPC分类号： C07D205/08 , C07D205/10 , C25B3/02
摘要： PURPOSE: To produce a 4-fluoro-2-azetidinone derivative by anodizing 4- trialkylsilyl-2-azetidinone as a substrate in the presence of fluorine ion. CONSTITUTION: Aldehyde is allowed to react with 1,3,4-trisilyl-azetidinone in the presence of a strong base to obtain a compd. shown by formula I (where R , R and R are each a straight or branched-chain 1-5C alkyl such as methyl, ethyl, isopropyl and isobutyl, R is a straight or branched-chain alkyl capable of having a substituent such as benzyl and phenetyl, R is hydrogen, the alkyl and an alkylidene group capable of having a substituent, and the broken line is a bond present in the case of alkylidene group). The compd. is anodized with triethylamine or the hydrofluoric acid salt of pyridine as a supporting electrolyte, and a 4-fluoro-2-azetidinone derivative shown by formula II is produced in high yield.

96. 发明专利

JPH07330721A PRODUCTION OF 2-AZETIDINONES 失效
公开(公告)号：JPH07330721A
公开(公告)日：1995-12-19
申请号：JP12098794
申请日：1994-06-02
申请人： SHIRATORI PHARM
发明人： ISOBE TOSHIO
IPC分类号： C07D205/08 , C07D403/04
摘要： PURPOSE:To provide a method for readily, industrially and advantageously producing 2-azetidinones useful as a medicine or a synthetic intermediate under nearly neutral mild conditions. CONSTITUTION:This method for producing 2-azetidinones of formula II [R to R are each an organic group), e.g. 1-(4-methoxyphenyl)-3-phenoxy-4- phenylazetidin-2-one is to react carboxylic acids having hydrogen atom at the alpha-position with imines in the presence of a base (e.g. pyridine or triethylamine) using a haloiminium salt of formula I [R and R are each a lower alkyl; X is a halogen; (n) is 2 or 3]. In the method, since the compound of formula I is converted into a water-soluble compound of formula III, the separation and purification can readily be carried out. The objective compound of formula II can simply be isolated according to a conventional method such as distillation or recrystallization. The compound of formula I is readily obtained by reacting the compound of formula III with a well-known halogenating agent.

97. 发明专利

JPH06247946A PRODUCTION OF 4-OXO-1,3-BENZOXAZINE COMPOUNDS 失效
公开(公告)号：JPH06247946A
公开(公告)日：1994-09-06
申请号：JP3193193
申请日：1993-02-22
申请人： SHIRATORI PHARM
发明人： ISOBE TOSHIO
IPC分类号： C07D265/22
摘要： PURPOSE:To produce the subject compound useful as a medicine, an agrochemical, etc., in a high yield by subjecting an N-acylanthranilic acid and an iminium halide salt to a dehydrative reaction. CONSTITUTION:An N-acylanthranilic acid of formula I (R , R are organic groups) is reacted with an iminium halide salt of formula II (R , R are lower alkyl ; X is halogen; (n) is 2,3) as a dehydrating agent in the presence of a base (e.g. triethylamine) in a solvent-free state or in a solvent (e.g. methylene chloride) at approximately room temperature to produce the objective compound of formula III. Approximately 1 mole of the compound of formula II and approximately 2 moles of the base are used per mole of the compound of formula I. The reaction can be performed under nearly neutral and mild conditions without being influenced by the properties of the compound of formula I. The compound of formula III includes 2-ethyl-4-oxo-1,3-benzoxazine.

98. 发明专利

JPH0586393B2 失效
公开(公告)号：JPH0586393B2
公开(公告)日：1993-12-10
申请号：JP1247885
申请日：1985-01-28
申请人： SHIRATORI PHARM , SUNTORY LTD
发明人： SAKAI HIDEAKI , KANAI SADA
IPC分类号： C07D475/04 , B01J31/00 , B01J31/28 , C07B61/00

99. 发明专利

JPH05202088A GLYCOSIDE AND ANTI-HEPATITIS AGENT CONTAINING THE SAME 失效
公开(公告)号：JPH05202088A
公开(公告)日：1993-08-10
申请号：JP41915790
申请日：1990-12-28
申请人： SHIRATORI PHARM
发明人： SAITO SADAO , NAGAMURA YOICHI , MIYAGAKI MITSUHIRO
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P1/16 , C07H15/256
摘要： PURPOSE:To provide a new glycoside capable of markedly inhibiting GOT activity and GPT activity, thus useful for antihepatitis agents having hepatopathy-inhibitory effects. CONSTITUTION:The.objective compound of formula I (either A or B is beta-D- glucuronopyranose, the other being,beta-D-glucopyranose or beta-D-galactopyranose). This compound can be obtained, for example, by the following method: a compound of formula II is made to react with a compound of formula III (Ac is acetyl; Bn is benzyl) under agitation in dry methylene chloride in the presence of cobalt bromide and trimethylsilyl chloride followed by treatment with NaOMe-MeOH to give a compound of formula IV; a compound of formula V is then added to the compound of the formula IV followed by further addition of silver trifluoromethanesulfonate, 1,1,3,3-tetramethylurea and 4Angstrom molecular sieve in dry methylene chloride and then agitation at room temperature to produce a compound of formula VI, which is, in turn, put to NaOMe-MeOH treatment, catalytic reduction, and KOH-MeOH treatment.

100. 发明专利

JPH0368594A PRODUCTION OF POLYNUCLEOTIDE 失效
公开(公告)号：JPH0368594A
公开(公告)日：1991-03-25
申请号：JP20654589
申请日：1989-08-09
申请人： SHIRATORI PHARM
发明人： TAKAKU HIROSHI , SAKAZUME OSAMU , YAMANE HIROSHI
IPC分类号： C07D233/28 , C07H21/04
摘要： PURPOSE:To obtain a polynucleotide in high yield and short time without causing side reaction by reacting a nucleoside phosphorous acid ester derivative with a nucleoside in the presence of an imidazolinium compound. CONSTITUTION:The objective polynucleoside is produced by condensing a nucleoside phosphorous acid ester derivative of formula I (A is pyrimidine base or purine base: R is hydroxyl-protecting group or mono or polynucleoside phosphorous acid ester residue; R is H or cationic group) with a nucleoside of formula II (B is pyrimidine base or purine base; R is same as R ) in the presence of an imidazolinium compound of formula III (R and R are lower alkyl; X and Y are halogen) in a solvent (e.g. acetonitrile) at room temperature and oxidizing the resultant polynucleoside phosphorous acid ester of formula IV. The amounts of the compound of formula I and the compound of formula III are 1-50mol and 1-250mol per 1 mol of the compound of formula II, respectively.

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