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1. 发明专利

DE3474829D1 PROCESS FOR AN ANTHRACYCLINE DERIVATIVE, AND AN ANTHRACYCLINONE DERIVATIVE USEFUL FOR THE PROCESS 未知
公开(公告)号：DE3474829D1
公开(公告)日：1988-12-01
申请号：DE3474829
申请日：1984-10-22
申请人： SAGAMI CHEM RES
发明人： TERASHIMA SHIRO , KIMURA YOSHIKAZU , SUZUKI MICHIYO , MATSUMOTO TERUYO , ABE RUMIKO
IPC分类号： C07F7/18 , C07H15/252 , C07C50/36
摘要： A process for producing an anthracycline derivative represented by the general formula:where R 1 is an acyl group, each of X 1 and X 2 is a hydrogen atom, a methoxy group, a hydroxyl group, a halogen atom or a lower alkyl group, each of Y 1 and Y 2 is a hydrogen atom, an alkoxy group or a hydroxyl group, and Z is a hydrogen atom or a protected hydroxyl group, which comprises reacting an anthracyclinone derivative represented by the general formula:where R is a hydrogen atom or a trialkylsilyl group, and X 1 , X 2 , Y 1 , Y 2 and Z are as defined above, with a 1-acylsugar derivative represented by the general formula:where R 2 is an acyl group and R 1 is as defined above, in the presence of a silyl sulfonic acid derivative represented by the general formula:where each of R 3 , R 4 and R 5 is an alkyl group and A is an alkyl group, an aryl group, a polyfluoroalkyl group or a hydrogen atom.

2. 发明专利

AT38233T 未知
公开(公告)号：AT38233T
公开(公告)日：1988-11-15
申请号：AT84112728
申请日：1984-10-22
申请人： SAGAMI CHEM RES
发明人： TERASHIMA SHIRO , KIMURA YOSHIKAZU , SUZUKI MICHIYO , MATSUMOTO TERUYO , ABE RUMIKO
IPC分类号： C07C50/36 , C07F7/18 , C07H15/252

3. 发明专利

JPH0481599B2 失效
公开(公告)号：JPH0481599B2
公开(公告)日：1992-12-24
申请号：JP19871984
申请日：1984-09-25
申请人： SAGAMI CHEM RES
发明人： TERAJIMA ATSURO , KIMURA YOSHIICHI , SUZUKI MICHO , ABE RUMIKO , MATSUMOTO MITSUYO
IPC分类号： C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P35/00

4. 发明专利

JPS6241588B2 失效
公开(公告)号：JPS6241588B2
公开(公告)日：1987-09-03
申请号：JP2805880
申请日：1980-03-07
申请人： SAGAMI CHEM RES
发明人： OSHIMA IWAO , SUGA SHIGEKI , ABE RUMIKO
IPC分类号： C07D205/08 , B01J23/00 , C07C67/00 , C07C231/00 , C07C231/10 , C07C235/20 , C07C235/32 , C07C235/34 , C07C235/38 , C07C237/30 , C07D205/085 , C07D209/18 , C07D213/56 , C07D307/54

5. 发明专利

JPS5643261A BETAALACTAM COMPOUND 失效
公开(公告)号：JPS5643261A
公开(公告)日：1981-04-21
申请号：JP11880079
申请日：1979-09-18
申请人： SAGAMI CHEM RES
发明人： OSHIMA IWAO , SUGA SHIGEKI , ABE RUMIKO
IPC分类号： C07D205/08 , C07D205/085
摘要： NEW MATERIAL:beta-Lactam compounds of formula I (R , R are H, lower alkyl, benzyl, acyl, or R and R may incorporate to form alkylene; R is alkyl, aryl, heteroaromatic group; X is amino, azide). EXAMPLE:1-Phenyl-3-azide-4-(3,4-dimethoxyphenyl)azetidin-2-one. USE:Synthetic intermediate of dopa, that is, a remedy for parkinson's diseases. When these compound are used as a starting material, dopa is obtained through shortened process in high yield. PREPARATION:The reaction of a Schiff base of formula II with an azide of formula III in the presence of a tertiary amine affords a compound of formula I', which is hydrogenolyzed in the presence of a catalyst such as Raney nickel to give a compound of formula I''.

6. 发明专利

JPH0348918B2 失效
公开(公告)号：JPH0348918B2
公开(公告)日：1991-07-25
申请号：JP12759084
申请日：1984-06-22
申请人： SAGAMI CHEM RES
发明人： TERAJIMA ATSURO , SUZUKI MICHO , KIMURA YOSHIICHI , ABE RUMIKO , MATSUMOTO MITSUYO , SHIOJIMA ISAO
IPC分类号： C07F7/08

7. 发明专利

JPS6124546A Preparation of alkyl 2-hydroxy-5,12-dimethoxy-1,2,3,4-tetrahydronaphthacene-6,11-dione-2-carboxylate 失效
标题翻译：烷基2-羟基-5,12-二甲基-1,2,3,4-四氢萘基-6,11-二酮-2-羧酸酯的制备
公开(公告)号：JPS6124546A
公开(公告)日：1986-02-03
申请号：JP14244684
申请日：1984-07-11
申请人： Sagami Chem Res Center
发明人： TERAJIMA ATSURO , KIMURA YOSHIICHI , SUZUKI MICHIYO , ABE RUMIKO , MATSUMOTO MITSUYO
IPC分类号： C07C69/757 , C07C67/08 , C07C67/31
摘要： PURPOSE: To obtain industrially and advantageously the titled compound, by esterifying 2,5,12-trihydroxy-1,2,3,4-tetrahydronaphthacene-6,11-dione-2-carboxylic acid, and methylating the resultant ester.
CONSTITUTION: A carboxylic acid expressed by formula I (X
1 and X
2 are H, OH, lower alkyl or halogen) is reacted with an alcohol expressed by the formula ROH (R is lower alkyl) in an aprotic polar solvent, e.g. dimethyl sulfoxide, in the presence of an acid, e.g. hydrochloric acid, to give a carboxylate expressed by formula II, which is then methylated to afford the aimed compound expressed by formula III. The above-mentioned methylation can be achieved by reaction of a methylating agent in an ordinary organic solvent, e.g. acetone, but must be carried out in the presence of a base in case a methyl halide or methyl sulfate is used as the methylating agent.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过酯化2,5,12-三羟基-1,2,3,4-四氢萘并-6,11-二酮-2-羧酸，得到工业上有利的标题化合物，并使所得酯甲基化。构成：由式I（X 1和X 2）表示的羧酸与H，OH，低级烷基或卤素表示的醇在非质子传递极性溶剂中与式ROH（R为低级烷基）表示的醇反应，例如二甲基亚砜，在酸的存在下，例如，盐酸，得到由式II表示的羧酸酯，然后将其甲基化，得到式III表示的目标化合物。上述甲基化可以通过甲基化剂在普通有机溶剂例如甲醇化反应中实现。丙酮，但必须在碱的存在下进行，以使用甲基卤或甲基硫酸盐作为甲基化剂。

8. 发明专利

JPS617231A Preparation of adriamycinone derivative 失效
标题翻译：阿德米霉醇衍生物的制备
公开(公告)号：JPS617231A
公开(公告)日：1986-01-13
申请号：JP12759384
申请日：1984-06-22
申请人： Sagami Chem Res Center
发明人： TERAJIMA ATSUROU , KIMURA YOSHIICHI , SUZUKI MICHIYO , ABE RUMIKO , MATSUMOTO MITSUYO
IPC分类号： C07C50/38 , C07C45/00 , C07C67/00
摘要： PURPOSE: To obtain an adriamycinone derivative useful as a raw material for adriamycins having improved carcinostatic actions by one stage in high purity in high yield, by treating a specific 14-halo derivative with an alkali by the use of an aqueous solvent of an aprotic amide.
CONSTITUTION: A 14-halo derivative shown by the formula I (R
1 is H, lower alkoxy, or OH; R
2 is H, or OH; X is Cl, Br, or I) such as 14-bromo-4-demethoxydaunomycinone that is easily obtained by halogenating a daunomycinone is treated with an alkali such as NaOH, NaHCO
3 , etc. in an aqueous solvent of an aprotic amide at 0°CW room temperature, to give the aimed compound shown by the formula II such as (+)-4-demethoxyadriamycinone, etc. Dimethylformamide, dimethylactamide, N-methylpyrrolidone, N-methylpiperidone, hexamethylphosphorotriamide, etc. may be cited as the aprotic amide.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过使用非质子酰胺的水性溶剂，通过用碱处理特定的14-卤代衍生物，得到可用作具有改善的高度纯度的一个阶段的具有改善的制癌作用的阿霉素的原料的阿霉素衍生物。构成：式I所示的14卤代衍生物（R 1是H，低级烷氧基或OH; R 2是H或OH; X是Cl，Br或I），例如14-溴在室温下，在非质子交换酰胺的水性溶剂中，用碱如NaOH，NaHCO 3等处理容易地通过卤化道诺霉素酮而得到的4-脱甲氧基多余霉素酮，得到目标化合物式（II）如（+） - 4-脱甲氧基对映体霉素等。可以列举二甲基甲酰胺，二甲基乳酰胺，N-甲基吡咯烷酮，N-甲基哌啶酮，六甲基磷酰三胺等。

9. 发明专利

JPS617229A Preparation of alpha-hydroxyketone derivative 失效
标题翻译： α-羟基酮衍生物的制备
公开(公告)号：JPS617229A
公开(公告)日：1986-01-13
申请号：JP12759184
申请日：1984-06-22
申请人： Sagami Chem Res Center
发明人： TERAJIMA ATSUROU , SUZUKI MICHIYO , KIMURA YOSHIICHI , ABE RUMIKO , MATSUMOTO MITSUYO , SHIOJIMA ISAO
IPC分类号： C07C45/00 , B01J23/00 , B01J23/06 , C07B61/00 , C07C45/42 , C07C49/573 , C07C49/577 , C07C49/727 , C07C49/753 , C07C67/00
CPC分类号： Y02P20/52
摘要： PURPOSE: To obtain the titled compound useful as an intermediate for synthesizing daunomycin, etc. by a simple reaction operation in high yield, by treating a specific naphthol derivative as a raw material in an acidic aqueous solution in the presence of a divalent mercuric ion.
CONSTITUTION: A 2-(2-trialkylsilylethynyl)-1,2,3,4-tetrahydro-2-naphtol derivative shown by the formula I [R
1 and R
4 are H, OH, or alkoxy; R
2 and R
3 are H or linked to form group shown by the formula II (X
1 and X
2 are R
1 , R
4 , lower alkyl, etc.); R
5 WR
7 are lower alkyl] is treated in an acidic aqueous solution in the presence of a mercuric ion such as mercuric oxide, etc. at room temperature for ≤ tens hours, to give the aimed compound shown by the formula III. The acidic aqueous solution is prepared from a mixed solution of an aqueous solution of a mineral acid such as 7W10 normal sulfuric acid, etc., an organic solvent, and water.
USE: An intermediate for synthesizing daunomycin, etc. that are an aglycone of anthracycline which is an aminoglycosdie antibiotic showing carcinostatic activity.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：通过在二价汞离子的存在下，通过在酸性水溶液中处理特定的萘酚衍生物作为原料，通过简单的高收率反应操作获得可用作合成道诺霉素等的中间体的标题化合物。构型：由式I [R 1和R 4]表示的2-（2-三烷基甲硅烷基乙炔基）-1,2,3,4-四氢-2-萘酚衍生物是H，OH或烷氧基; R 2和R 3是H或连接到式II所示的基团（X 1和X 2是R 1，R 4，低级烷基等）; R 5 -R 7是低级烷基]在酸性水溶液中，在汞离子如氧化汞等的存在下在室温下处理<=数十小时，得到目标化合物公式三。酸性水溶液由无机酸水溶液如7-10正硫酸等与有机溶剂和水的混合溶液制备。用途：合成道诺霉素等的中间体，它是作为氨基糖应激抗生素的蒽环素的糖苷配基，具有显着的致癌活性。

10. 发明专利

JPS56125360A BETA-LACTAM COMPOUND 失效
公开(公告)号：JPS56125360A
公开(公告)日：1981-10-01
申请号：JP2805780
申请日：1980-03-07
申请人： SAGAMI CHEM RES
发明人： OSHIMA IWAO , SUGA SHIGEKI , ABE RUMIKO
IPC分类号： C07D205/08 , C07D205/085 , C07D401/04 , C07D403/04 , C07D405/04 , C07D407/04 , C07D409/04
摘要： NEW MATERIAL:Compounds of formula I' and formula I'' [Ar is heteroaromatic group or group of formula p-Y>C6H4 (Y is F, OH, or protected OH); R is alkyl, aryl, etc.; X' is benzyloxy or azido; X'' is OH or amino, provided that when x' is azido, Ar is not p-fluorophenyl]. EXAMPLE:1-Phenyl-3-azido-4-(2'-furyl)azetidin-2-one. USE:Intermediate for the preparation of useful animal growth promoter, etc. PROCESS:Reaction of a Schiff base of formula II with a compound of formula III in a solvent such as benzene in the presence of a tert-amine such as triethylamine at -78-+100 deg.C affords a compound of formula I', which is converted to a compound of formula I'' by the hydrogenative decomposition in a solvent such as methanol, in the presence of a catalyst such as Pd black at room temp. -150 deg.C.

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