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51. 发明专利

JPS6429390A PRODUCTION OF PENTOFURANOSIDE DERIVATIVE 失效
公开(公告)号：JPS6429390A
公开(公告)日：1989-01-31
申请号：JP18366287
申请日：1987-07-24
申请人： ASAHI GLASS CO LTD
发明人： MORISAWA YOSHITOMI , ASAI TOMOYUKI , YASUDA ARATA , UCHIDA KEIICHI
IPC分类号： C07H19/06 , C07H5/02 , C07H19/16
摘要： PURPOSE:To obtain the titled compound useful as medicines, agricultural chemicals, etc., such as metabolic antagonistic substance, RNA synthesis inhibitor, antitumor agent or antiviral agent, by converting a specific group in a deoxy-fluoropentofuranoside derivative into H atom. CONSTITUTION:The -OX group in a 3-deoxy-3-fluoropentofuranoside derivative expressed by formula I [R is halogen, -OZ (Z is alkyl or OH-protecting group) or residue of nucleic acid bases which may have a protecting group; R is OH- protecting group; X is H or eliminative activating group] is converted into H atom to afford the aimed compound expressed by formula II. Furthermore, the -OX group is preferably converted into the H atom by using a reducing agent, such as tributyltin hydride or triphenyltin hydride.

52. 发明专利

JPS62242693A FLUORINE-CONTAINING RIBOFURANOSIDE DERIVATIVE AND PRODUCTION THEREOF 失效
公开(公告)号：JPS62242693A
公开(公告)日：1987-10-23
申请号：JP8494086
申请日：1986-04-15
申请人： ASAHI GLASS CO LTD
发明人： UCHIDA KEIICHI , YASUDA ARATA , MORISAWA YOSHITOMI
IPC分类号： C07H5/02 , C07H15/04 , C07H19/06 , C07H19/16
摘要： NEW MATERIAL:2,3-Dideoxy-2,3-difluoro-D-ribofuranoside derivative of formula I [R is halogen, -OX (X is H, alkyl or protecting group) or residue of nucleic acid base; R is H or protecting group]. EXAMPLE:Methyl 2,3-dideoxy-2,3-difluoro-5-O-benzyl-beta-D-ribofuranoside. USE:A metabolism antagonistic agent. PREPARATION:A fluororibofuranoside derivative of formula II (R is alkoxy or halogen; R is protecting group; Y is H or eliminable group) is fluorinated to introduce F atom at 2-position. If necessary, the product is subjected to deprotection, introduction of nucleic acid base, etc.

53. 发明专利

JPS62240693A RIBOFURANOSIDE DERIVATIVE AND PRODUCTION THEREOF 失效
公开(公告)号：JPS62240693A
公开(公告)日：1987-10-21
申请号：JP8231586
申请日：1986-04-11
申请人： ASAHI GLASS CO LTD
发明人： UCHIDA KEIICHI , YASUDA ARATA , MORISAWA YOSHITOMI
IPC分类号： C07H5/02 , C07H15/04 , C07H19/06 , C07H19/16
摘要： NEW MATERIAL:A 3,5-dideoxy-3,5-difluoro-D-ribofuranoside derivative expressed by formula I [R represents halogen atom, -OX (X represents H, alkyl or protect ing group) or residue of nucleic acid bases; R represents H or protecting group]. EXAMPLE:Methyl 2-O-benzyl-3,5-dideoxy-3,5-difluoro-beta-D-ribofuranoside. USE:An antiviral agent and antitumor agent. PREPARATION:A fluororibofuranoside derivative expressed by formula II (R represents alkoxyl or halogen atom; R represents protecting group Z represents H or eliminating group) is fluorinated to introduce a fluorine atom into the 5-th position. Then, if necessary, deprotection, introduction of nucleic acid bases, etc., are carried out.

54. 发明专利

JPS61254537A GAMMA-FLUORO-ALPHA-HYDROXYCARBOXYLIC ACID DERIVATIVE AND PRODUCTION THEREOF 失效
公开(公告)号：JPS61254537A
公开(公告)日：1986-11-12
申请号：JP9355685
申请日：1985-05-02
申请人： ASAHI GLASS CO LTD
发明人： UCHIDA KEIICHI , YASUDA ARATA , MORISAWA YOSHITOMI
IPC分类号： C07C59/115 , C07C51/00 , C07C51/367 , C07C59/56 , C07C67/00 , C07C67/31 , C07C69/675 , C07C69/732
摘要： NEW MATERIAL:A gamma-fluoro-alpha-hydroxycarboxylic acid derivative shown by the formula I (Rf is fluoroalkyl containing one or more F at 1-position; R and R are alkyl, cycloalkyl, aryl or aralkyl and R is further H). EXAMPLE:(2S,3S)-2-Hydroxy-3-methyl-4,4,4-trifluorobutanoic acid ethyl ester. USE:An intermediate capable of synthesizing highly stereospecifically a fluorine- containing amino acid useful as a physiologically active substance, especially gamma-fluorovaline. PREPARATION:A compound shown by the formula II (R is each group among R ) is reacted with an alkali metallic amide, reacted with an electrophilic reagent, and optionally hydrolyzed to give stereospecifically a compound shown by the formula I.

55. 发明专利

JPS61254533A PRODUCTION OF ALPHA-SUBSTITUTED-GAMMA-FLUOROCARBONYL COMPOUND 失效
公开(公告)号：JPS61254533A
公开(公告)日：1986-11-12
申请号：JP9355785
申请日：1985-05-02
申请人： ASAHI GLASS CO LTD
发明人： UCHIDA KEIICHI , YASUDA ARATA , MORISAWA YOSHITOMI
IPC分类号： C07C45/64 , C07B31/00 , C07B37/04 , C07B41/02 , C07B41/04 , C07B45/06 , C07B47/00 , C07C45/00 , C07C45/68 , C07C45/72 , C07C49/167 , C07C49/173 , C07C67/00 , C07C67/31 , C07C67/343 , C07C69/62 , C07C69/67 , C07C227/00 , C07C227/06 , C07C227/12 , C07C229/12 , C07C313/00 , C07C319/14 , C07C323/22 , C07C323/52 , C07C325/00 , C07C391/00
摘要： PURPOSE:To obtain the titled substance useful as an intermediate for a physiologically active substance, by reacting a gamma-fluorocarbonyl compound with an alkali metallic amide to give an alkali metallic enolate and reacting it with an electrophilic reagent. CONSTITUTION:A compound shown by the formula I [Rf is fluoroalkyl containing at least one F atom at 1-position; R is alkyl, cycloalkyl, aryl, etc.; X is -O-R or -R (R is alkyl, cycloalkyl, aryl, etc.)] is reacted with an alkali metallic amide to give an alkali metallic enolate shown by the formula II, which is treated with an electrophilic reagent (e.g., aliphatic ketone, aliphatic aldehyde or iodated N,N-dialkylmethylene ammonium) in a solvent such as THF, etc., preferably at

56. 发明专利

JPS6121455B2 JPS6121455B2 - 失效
公开(公告)号：JPS6121455B2
公开(公告)日：1986-05-27
申请号：JP15416178
申请日：1978-12-15
申请人： Asahi Glass Co Ltd
发明人： UCHIDA KEIICHI , MORIKAWA SHINSUKE , ODA YOSHIO
IPC分类号： C07D239/553 , C07B31/00 , C07B39/00 , C07C17/00 , C07C17/12 , C07C25/13 , C07C41/00 , C07C41/22 , C07C43/12 , C07C67/00 , C07C201/00 , C07C201/12 , C07C205/12 , C07D239/54

57. 发明专利

JPS6178724A Antitumor agent 失效
标题翻译：抗菌剂
公开(公告)号：JPS6178724A
公开(公告)日：1986-04-22
申请号：JP19856384
申请日：1984-09-25
申请人： Asahi Glass Co Ltd , Kirin Brewery Co Ltd , Tetsuo Suami
发明人： SUAMI TETSUO , YONESHIMA NOBUYASU , UCHIDA KEIICHI
IPC分类号： A61K31/17 , A61P35/00
摘要： PURPOSE: To provide an antitumor agent composed of a specific nitrosourea derivative having 2-fluoroethyl group, acting as an alkylation agent similar to a compound having 2-chloroethyl group, and having widened applicable therapeutic field.
CONSTITUTION: The nitrosourea derivative of formula A or its salt is used as an antitumor agent. It has been found newly that the compound of formula A acts as an alkylation agent similar to the compound having 2-chloroethyl group. It has wider therapeutic range as an antitumor agent than compound having 2-chloroethyl group, and is applicable to wide variety of diseases. The compound of formula A can be prepared by reacting the compound of formula B with the compound of formula C.
COPYRIGHT: (C)1986,JPO&Japio
摘要翻译：目的：提供由具有2-氟乙基的特异性亚硝基脲衍生物构成的抗肿瘤剂，作为与具有2-氯乙基的化合物类似的烷基化剂，并具有扩大的适用治疗领域。构成：将式A的亚硝基脲衍生物或其盐用作抗肿瘤剂。已经发现，式A化合物作为类似于具有2-氯乙基的化合物的烷基化剂起作用。与具有2-氯乙基的化合物相比，作为抗肿瘤剂具有更广泛的治疗范围，适用于多种疾病。式A的化合物可以通过使式B化合物与式C化合物反应来制备。

58. 发明专利

JPS615477B2 JPS615477B2 - 失效
公开(公告)号：JPS615477B2
公开(公告)日：1986-02-18
申请号：JP14400977
申请日：1977-12-02
申请人： Asahi Glass Co Ltd
发明人： ODA YOSHIO , UCHIDA KEIICHI , MORIKAWA SHINSUKE
IPC分类号： C07D239/22 , C07D239/54 , C07D239/553
摘要： PURPOSE:To obtain the title compound useful as a raw material for various medicines, e.g. oncostatic drugs, etc. with a high utilization of gas at a high selectivity industrially advantageously, by reacting orotic acid with fluorine gas in an available formic acid medium. CONSTITUTION:Fluorine gas diluted to 0.5-50 times, preferably 1-10 times, with an inert gas is reacted with orotic acid in formic acid at 5-50 deg.C to give an intermediate product (adduct) of formula I, which is then heated in water at 90 deg.C or above, or in air at 100-160 deg.C to form 5-fluoro orotic acid of formula II. The molar dilution ratio of formic acid to orotic acid is 1-1,000:1, preferably 20-100:1.

59. 发明专利

JPS5924983B2 JPS5924983B2 - 失效
公开(公告)号：JPS5924983B2
公开(公告)日：1984-06-13
申请号：JP12884975
申请日：1975-10-28
申请人： Asahi Glass Co Ltd
发明人： ODA YOSHIO , UCHIDA KEIICHI , MORIKAWA SHINSUKE
IPC分类号： C07D303/48 , B01J23/00 , B01J23/72 , B01J27/00 , B01J27/10 , C07B61/00 , C07D301/08 , C07D303/08
CPC分类号： Y02P20/52

60. 发明专利

JPS5917087B2 JPS5917087B2 - 失效
公开(公告)号：JPS5917087B2
公开(公告)日：1984-04-19
申请号：JP12885175
申请日：1975-10-28
申请人： Asahi Glass Co Ltd
发明人： ODA YOSHIO , UCHIDA KEIICHI , MORIKAWA SHINSUKE
IPC分类号： C07D303/48 , B01J27/00 , C07B61/00 , C07D301/08 , C07D303/08
CPC分类号： Y02P20/52

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