JPS5791995A - Nucleoside-5'-o-morpholinoacyl ester and its preparation - Google Patents

Nucleoside-5'-o-morpholinoacyl ester and its preparation

Info

Publication number
JPS5791995A
JPS5791995A JP56080228A JP8022881A JPS5791995A JP S5791995 A JPS5791995 A JP S5791995A JP 56080228 A JP56080228 A JP 56080228A JP 8022881 A JP8022881 A JP 8022881A JP S5791995 A JPS5791995 A JP S5791995A
Authority
JP
Japan
Prior art keywords
nucleoside
ester
expressed
morpholinoacyl
formulai
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP56080228A
Other languages
Japanese (ja)
Inventor
Takeshi Endo
Katsumi Sakai
Kiyoaki Cho
Yoshitaka Inamoto
Haruhiko Teshigahara
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Fuji Chemical Industries Co Ltd
Original Assignee
Fuji Chemical Industries Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US06/210,796 external-priority patent/US4340728A/en
Application filed by Fuji Chemical Industries Co Ltd filed Critical Fuji Chemical Industries Co Ltd
Publication of JPS5791995A publication Critical patent/JPS5791995A/en
Pending legal-status Critical Current

Links

Classifications

    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

NEW MATERIAL:A nucleoside-5'-O-morpholinoacyl ester expressed by formulaI (A is an acyl group of a saturated fatty acid having a morpholino group at the α- or ω-position; Z and Z' are H or OH, however not OH at the same time).
EXAMPLE: 5'-O-(5-Morpholinopentanoyl)-5-fluorouidine.
USE: An antimalignant tumor agent, antiviral agent and immunological inhibitor.
PROCESS: A saturated fatty acid having a morpholino group at the α- or the ω- position is esterified with a nucleoside expressed by formula II e.g. 5-fluorouridine, in an anhydrous solvent, e.g. benzene or chloroform, in the presence of a basic compound, e.g. a trialkylamine or pyridine, and a condensing agent, e.g. p-toluenesulfonyl chloride, at 40°C or below to form an ester bond and give the compound expressed by formulaI.
COPYRIGHT: (C)1982,JPO&Japio
JP56080228A 1980-11-26 1981-05-28 Nucleoside-5'-o-morpholinoacyl ester and its preparation Pending JPS5791995A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US06/210,796 US4340728A (en) 1979-11-28 1980-11-26 Nucleoside derivatives and process for preparing same

Publications (1)

Publication Number Publication Date
JPS5791995A true JPS5791995A (en) 1982-06-08

Family

ID=22784293

Family Applications (5)

Application Number Title Priority Date Filing Date
JP56079434A Pending JPS5791994A (en) 1980-11-26 1981-05-27 5'-o-(n-alkylcarbamoylalanyl)-5-fluorouridine and its preparation
JP56080228A Pending JPS5791995A (en) 1980-11-26 1981-05-28 Nucleoside-5'-o-morpholinoacyl ester and its preparation
JP56080229A Granted JPS5791996A (en) 1980-11-26 1981-05-28 Novel nucleoside derivative and its preparation
JP56080231A Pending JPS5791998A (en) 1980-11-26 1981-05-28 Novel 5'-o-acylnucleoside derivative and its preparation
JP56080230A Granted JPS5791997A (en) 1980-11-26 1981-05-28 5'-o-acylnucleoside and its preparation

Family Applications Before (1)

Application Number Title Priority Date Filing Date
JP56079434A Pending JPS5791994A (en) 1980-11-26 1981-05-27 5'-o-(n-alkylcarbamoylalanyl)-5-fluorouridine and its preparation

Family Applications After (3)

Application Number Title Priority Date Filing Date
JP56080229A Granted JPS5791996A (en) 1980-11-26 1981-05-28 Novel nucleoside derivative and its preparation
JP56080231A Pending JPS5791998A (en) 1980-11-26 1981-05-28 Novel 5'-o-acylnucleoside derivative and its preparation
JP56080230A Granted JPS5791997A (en) 1980-11-26 1981-05-28 5'-o-acylnucleoside and its preparation

Country Status (1)

Country Link
JP (5) JPS5791994A (en)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5925327A (en) * 1982-07-31 1984-02-09 Hidematsu Hirai Preparation of antitumor complex
JPS63196519A (en) * 1987-02-12 1988-08-15 Mitsui Toatsu Chem Inc Carcinostatic agent
US5470838A (en) * 1987-10-28 1995-11-28 Pro-Neuron, Inc. Method of delivering exogenous uridine or cytidine using acylated uridine or cytidine
US5583117A (en) * 1987-10-28 1996-12-10 Pro-Neuron, Inc. Acylated uridine and cytidine for elevating tissue uridine and cytidine
US5783689A (en) * 1996-11-12 1998-07-21 University Of Notre Dame Antibacterial and antifungal nucleosides
US6020320A (en) * 1987-10-28 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US6020322A (en) * 1993-11-09 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US7169765B1 (en) 1988-10-27 2007-01-30 Wellstat Therapeutics Corporation Acyl deoxyribonucleoside derivatives and uses thereof

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS61134397A (en) * 1984-12-01 1986-06-21 Fuji Kagaku Kogyo Kk 5'-o-oligopeptidyl-5-fluorouridine and production thereof
WO1987007276A1 (en) * 1986-05-30 1987-12-03 Fuji Kagaku Kogyo Kabushiki Kaisha Novel 5-fluorouridine compounds and process for their preparation
AU610913B2 (en) * 1987-07-31 1991-05-30 Taiho Pharmaceutical Co., Ltd. 2'-deoxy-5-fluorouridine derivatives
JP2631227B2 (en) * 1988-07-11 1997-07-16 大鵬薬品工業株式会社 5'-benzyl-5-fluorouridine derivatives and intermediates thereof
WO1991012259A1 (en) * 1990-02-08 1991-08-22 Sankyo Company, Limited 5-fu derivative
JP2526414B2 (en) * 1994-05-20 1996-08-21 工業技術院長 Anticancer drug ester compound and method for producing the same

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5925327A (en) * 1982-07-31 1984-02-09 Hidematsu Hirai Preparation of antitumor complex
JPH0449524B2 (en) * 1982-07-31 1992-08-11 Hidematsu Hirai
JPS63196519A (en) * 1987-02-12 1988-08-15 Mitsui Toatsu Chem Inc Carcinostatic agent
US6020320A (en) * 1987-10-28 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US5583117A (en) * 1987-10-28 1996-12-10 Pro-Neuron, Inc. Acylated uridine and cytidine for elevating tissue uridine and cytidine
US5470838A (en) * 1987-10-28 1995-11-28 Pro-Neuron, Inc. Method of delivering exogenous uridine or cytidine using acylated uridine or cytidine
US6103701A (en) * 1987-10-28 2000-08-15 Von Borstel; Reid Warren Method for enhancing hematopoiesis with acyl deoxyribonucleosides
US6258795B1 (en) 1987-10-28 2001-07-10 Pro-Neuron, Inc. Acylated uridine and cytidine and uses thereof
US6274563B1 (en) 1987-10-28 2001-08-14 Pro-Neuron, Inc. Acylated uridine and cytidine and uses thereof
US6297222B1 (en) 1987-10-28 2001-10-02 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US6306834B1 (en) 1987-10-28 2001-10-23 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US6316426B1 (en) 1987-10-28 2001-11-13 Pro-Neuron, Inc. Acylated uridine and cytidine and uses thereof
US7169765B1 (en) 1988-10-27 2007-01-30 Wellstat Therapeutics Corporation Acyl deoxyribonucleoside derivatives and uses thereof
US6020322A (en) * 1993-11-09 2000-02-01 Pro-Neuron, Inc. Acyl deoxyribonucleoside derivatives and uses thereof
US5783689A (en) * 1996-11-12 1998-07-21 University Of Notre Dame Antibacterial and antifungal nucleosides

Also Published As

Publication number Publication date
JPS5791998A (en) 1982-06-08
JPS6247198B2 (en) 1987-10-06
JPS5791997A (en) 1982-06-08
JPS5791994A (en) 1982-06-08
JPS6247196B2 (en) 1987-10-06
JPS5791996A (en) 1982-06-08

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