Synthesis and Biological Evaluation of Phosphonopyrimidine and Phosphonopurine Ribonucleosides(Medeicinal Chemistry,Chemical)

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概要

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• Treatment oflithiated 2',3',5'-tri-О-protected uridine and 6-chloropurine ribonueleoside with diethyl chlorophosphate, followed by deblocking (and amination) and hydrolysis, provided 5- and 6-phosphonouridine (IV and VII), and 8-phosphonoadenosine (Xb), respectively. The Arbuzov reaction of 2',3',5'-tri-О-protected 4-chloro-2(1H)-pyrimidinone ribonucleoside and triethyl phosphite afforded the diethyl 4-phosphonatc derivative (XII). Compounds IV, VII and Xb, and their respective diethyl esters (IIb and VIb) and monoethyl ester (Xa) were inactive in vitro as antiviral and cytostatic agents, but the diethyl 8-phosphonate derivative (IXb) of 6-chloro-9-(β-D-ribofuranosyl)purine (VIIIa) showed some antiviral and cytostatic activities, which were comparable in all respects to those of VIIIa.

• 公益社団法人日本薬学会の論文
• 1987-08-25

著者

• BALZARINI Jan

  Rega Institute for Medical Research, Katholieke Universiteit Leuven

• CLERCQ Erik

  Rega Institute for Medical Research, Katholieke Universiteit Leuven

• MARUYAMA Tokumi

  Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University

• Blanco Jose

  Departamento De Farmacologia Facultade De Farmacia Universidade De Santiago De Compostela

• Clercq Erik

  Rega Instituut Katholieke Universiteit Leuven

• Clercq Erik

  Rega Institute For Medical Research Katholieke Universiteit Leuven

• Balzarini J

  Rega Inst. For Medical Res.

• HONJO MIKIO

  Faculty of Pharmaceutical Sciences, Tokushima Bunri University

• HORIKAWA MITZUYO

  Faculty of Pharmaceutical Sciences, Tokushima Bunri University

• Maruyama Tokumi

  Fac. Of Pharmaceutical Sciences At Kagawa Campus Tokushima Bunri Univ.

• Maruyama Tokumi

  Faculty Of Pharmaceutical Sciences At Kagawa Campus Tokushima Bunri University

• Balzarini Jan

  Rega Inst. For Medical Res.

• Balzarini J

  Rega Institute For Medical Research Katholieke Universiteit Leuven

• Honjo M

  Tokushima Bunri Univ. Tokushima

• Horikawa Mitzuyo

  Faculty Of Pharmaceutical Sciences Tokushima Bunri University

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