SYNTHESIS OF ACYCLIC NUCLEOSIDE DERIVATIVES

Novel intermediates and improvements in the synthesis of acyclic guanine nucleoside prodrugs of the formula (R)-9-[(2-alkanoylmethyl)-4- (aminoacyloxy)butyl]guanine (for example valtamociclovir stearate), including purine salts amenable to one pot alkylation with the acyclic side chain, acyclic 2-am...

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Hauptverfasser: TIAN, ZHENPING, WAYNE, GREG, ZHANG, WEIJIANG, RILEY, DAVID A, CURTY, CYNTHIA B, PLATA, DANIEL, LEANNA, M. ROBERT, PATEL, RAMESH R, LANNOYE, GREG, TIEN, JIEN-HEH J, NARAYANAN, BIKSHANDARKOIL A, SHELAT, BHADRA, CHANG, SOU-JEN, BELLETTINI, JOHN, LUKIN, KIRILL A, RASMUSSEN, MICHAEL, KOLACZKOWSKI, LAWRENCE, HANNICK, STEVEN M, SINGAM, PULLA REDDY, MORTON, HOWARD, BHAGAVATULA, LAKSHMI, YANG, CHENG-XI, GATES, BRADLEY D, SPITZ, TIFFANY
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:Novel intermediates and improvements in the synthesis of acyclic guanine nucleoside prodrugs of the formula (R)-9-[(2-alkanoylmethyl)-4- (aminoacyloxy)butyl]guanine (for example valtamociclovir stearate), including purine salts amenable to one pot alkylation with the acyclic side chain, acyclic 2-amino-6-halo-purine and protected guanine precursors, one pot manipulations thereof and last step work up procedures.