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公开(公告)号：JPH06157394A
公开(公告)日：1994-06-03
申请号：JP4338691
申请日：1991-03-08
发明人： TAKEUCHI TOMIO , AOYANAGI TAKAAKI , TATEE TOCHIROU , SHIMADA NOBUYOSHI , ABE FUMINORI , MURAOKA YASUHIKO , AOYAMA TAKAYUKI
IPC分类号： C07C45/65 , C07C49/737
摘要： PURPOSE:To obtain benastatin C and D especially useful as an immunopotentiator, having immunomodulating action, in high yield by decarboxylating benastatin C and D of specific structure in the presence of a reaction promoter in an inert solvent. CONSTITUTION:Streptomyces sp. M1,384-DF12 strain (FERM P-3,228) is inoculated into a medium, subjected to shaking culture at 27 deg.C for 4 days, the culture solution is filtered and the culture filtrate is separated from the cells by fraction. The culture solution is extracted with ethyl acetate, the extracted solution is concentrated to give a red crude substance, which is dissolved in methanol and purified by silanized silica get chromatography to give benastatin A and D of formula I (R is CH=CH or CH2CH2). Then the compound is decarboxylated in the presence of a reaction promoter such as copper sulfate in an inert solvent such as quinoline under heating at 120-200 deg.C to give the benastatin C and D of formula II useful as an immunomodulator.
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公开(公告)号：JPH0565520B2
公开(公告)日：1993-09-17
申请号：JP11915388
申请日：1988-05-18
申请人： NIPPON KAYAKU KK
发明人： SHIMADA NOBUYOSHI , HASEGAWA SHIGERU , TOMIZAWA TAKAYUKI , SAITO SEIICHI , SHIBUYA KYOICHI , FUJII AKIO , HOSHINO KORO
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P31/12 , A61P37/06 , C07D405/14 , C07D473/16 , C07H19/16 , C12P19/40 , C12R1/05 , C12R1/19 , C12R1/365 , C12R1/37 , C12R1/465 , C12R1/47 , C12R1/50 , C12R1/58 , C12R1/685 , C12R1/77 , C12R1/82
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公开(公告)号：JPH05194307A
公开(公告)日：1993-08-03
申请号：JP30761191
申请日：1991-11-22
发明人： TAKEUCHI TOMIO , AOYANAGI TAKAAKI , TATEE TOCHIROU , SHIMADA NOBUYOSHI , MURAOKA YASUHIKO , AOYAMA TAKAYUKI
摘要： PURPOSE:To obtain bequinostatin B having immunomodulating action and expected to be useful especially as an immunoactivating agent from bequinostatin A in high yield. CONSTITUTION:Carboxyl group of bequinostatin A of formula I which is a main component of a fermentation product of Streptomyces sp. MI384-DF12 strain (FERM BP-3228) is eliminated by decarboxylation reaction to obtain a large amount of bequinostatin B of formula II which is a minor component of the above fermentation product. The decarboxylation reaction is carried out in a solvent (preferably in a polar solvent such as quinoline, isoquinoline, aniline and/or water) or in the absence of solvent (especially preferably in quinoline) in ordinary atmosphere or a non-oxidizing atmosphere (e.g. in nitrogen, helium or argon) preferably at 40-500 deg.C (especially 80-300 deg.C) optionally under pressure.
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公开(公告)号：JPH03183491A
公开(公告)日：1991-08-09
申请号：JP32250789
申请日：1989-12-14
申请人： NIPPON KAYAKU KK
摘要： PURPOSE:To obtain the subject compound which is an antibiotic substance in a large production by adding a nutrient culture medium containing a nucleic acid substance added thereto and culturing a microorganism capable of producing oxetanocin A therein. CONSTITUTION:A microorganism [e.g. (Bacillus megaterium) NK84-0218] capable of producing oxetanocin A is cultured in a nutrient culture medium containing preferably 0.01-0.1% nucleic acid substance (e.g. nucleic acid base, nucleoside or nucleotide) added thereto at, e.g. 27 deg.C to afford the objective compound.
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公开(公告)号：JPH0363290A
公开(公告)日：1991-03-19
申请号：JP19947289
申请日：1989-08-02
申请人： NIPPON KAYAKU KK
IPC分类号： C07H19/16 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P31/12
摘要： PURPOSE:To obtain the subject compound useful as an antiviral agent by reacting a specific oxetanosine derivative with a carboxylic acid salt and removing protecting group, etc., from the reaction product. CONSTITUTION:The objective compound of formula V can be produced by reacting an oxetanosine derivative of formula I [P1 is protecting group; R1 is (substituted) lower alkylsulfonyl or (substituted) arylsulfonyl; B is purine base residue having protected functional group] [e.g. the compound of formula II (Bz is benzoyl; Tf is trifluoromethanesulfonyl)] with a carboxylic acid salt (e.g. sodium benzoate) and removing the protecting group and group R2 from the resultant compound of formula III (R2 is organic carbonyl) (e.g. the compound of formula IV).
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公开(公告)号：JPH02279693A
公开(公告)日：1990-11-15
申请号：JP9890789
申请日：1989-04-20
申请人： NIPPON KAYAKU KK
IPC分类号： C07H19/16 , C07D473/34
摘要： PURPOSE:To readily prepare the subject compound in a large amount by hydrolyzing an alkoxylated 2-aminooxetanosine A to remove the alkoxy group. CONSTITUTION:Oxetanosine-A(OXT-A) is subjected to an N-oxidation and subsequently to the introduction of a cyano group to the amino group through an oxadiazole ring to prepare a cyanated N-oxide OXT-A of formula I useful as an intermediate for the preparation of the 2-OXT-A. The compound of formula I is alkylated to prepare a cyanated N-alkoxy OXT-A of formula II (R1 is lower alkyl) and subsequently subjected to an alkali treatment, a neutralization and heating treatment to provide a compound of formula III. The compound of formula III is reacted in the presence of a catalyst such as a palladium catalyst in a polar solvent such as methanol or a mixture thereof with water under 1 to 20 atmospheres at 0 to 150 deg.C for 1 to 10hr to provide the objective compound. The compound may be, if necessary, crystallized to form an acid salt thereof by adding an acid and a solvent to aqueous suspension thereof.
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公开(公告)号：JPS62210998A
公开(公告)日：1987-09-17
申请号：JP5150386
申请日：1986-03-11
申请人： NIPPON KAYAKU KK
摘要： PURPOSE:To obtain minimycin having antimicrobial and carcinostatic action by a novel excellent method, by cultivating a specific microorganism belonging to the genus Streptomyces. CONSTITUTION:Streptomyces sp. NK83-0153 (FERM-P No.7317) is cultivated in a culture medium. The microorganism is collected from soil in OKUTAMA Mountains, Tokyo Metropolis and characterized by forming psudosporangium in sucrose nitrate agar culture medium. A cultivation method for actinomyces applies correspondingly to this method for cultivating the microorganism, but a submerged cultivation method by liquid culture is advantageous.
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公开(公告)号：JPH08311049A
公开(公告)日：1996-11-26
申请号：JP3015096
申请日：1996-01-25
申请人： NIPPON KAYAKU KK
IPC分类号： C07D263/24
摘要： PURPOSE: To obtain the subject new compound useful as a raw material for an intermediate for synthesizing a medicine such as bestatin, a curing agent for leukemia or a reagent. CONSTITUTION: This is an L-threo-β-hydroxyaspartic aid derivative of the formula (R1 and R2 are each H or a protecting group for a carboxyl), e.g. L-threo-β- hydroxyaspartic acid oxazolidone or (4S, 5S)-5-methoxycarbonyl-4- benzyloxycarbonyl oxazolidone. A compound of the formula is obtained e.g. by treating (A) L-threo-β-hydroxyaspartic acid diester with (B) a phosgene (especially preferably phosgene dimer) in an inert solvent to obtain an L-threo-β- hydroxyaspartic acid oxazolidone derivative or by subsequently deblocking a carboxyl-protecting group.
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公开(公告)号：JPH06192266A
公开(公告)日：1994-07-12
申请号：JP35724192
申请日：1992-12-24
申请人： NIPPON KAYAKU KK
发明人： SHIMADA NOBUYOSHI , YAMASHITA TAKUMI , SUGI KAZUTO , OKADA MINEAKI , TAKEUCHI TOMIO , TATSUTA KUNIAKI
IPC分类号： A61K31/365 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P27/02 , A61P35/00 , C07D493/20 , C07H17/08 , C12P17/18 , C12R1/465 , A61K31/71
摘要： PURPOSE:To obtain a new compound useful as a chemotherapeutic agent for malignant tumors, or a preventive/treating agent for the diseases involving vascular hyperplasia. CONSTITUTION:The compound o the formula [R and R are each H, (substituted)acyl or (substituted)saccharide; where, R and R are not H at the same time], e.g. 9-O-(4-dimethylaminobutyl)NK86-0279-I. The compound of the formula can be obtained, for example, by acylating NK86-0274-I with a cyclic diacarboxylic anhydride such as succinic anhydride or maleic anhydride in the presence of an organic base such as pyridine.
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