【発明の名称】ジヌクレオチド及びオリゴヌクレオチドアナログのための中間体

Japanese Patent JPH10506621

A

PCT No. PCT/GB95/01955 Sec. 371 Date Apr. 14, 1997 Sec. 102(e) Date Apr. 14, 1997 PCT Filed Aug. 17, 1995 PCT Pub. No. WO96/08503 PCT Pub. Date Mar. 21, 1996A compound of formula (I) or salts thereof, where R0 is hydrogen or together with R7O denotes a C1-C15 hydrocarbylidenedioxy group, R1 is hydrogen, R1a or a group of formula (II), R1a is R1b or a protecting group Q, R1b is C1-C20 alkyl, C2-C20 alkenyl, C3-C10 cycloalkyl, C6-C15 aryl, C7-C16 aralkyl or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R2 is R2a or -OR15 or together with R5 denotes an oxy group -O-, provided that R2 is -OR15 when R1 is a group of formula (II), R2a is a C1-C20 aliphatic group, a C3-C10 cycloaliphatic group, a C6-C15 aromatic group, a C7-C16 araliphatic group, or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R3 is R3a or Z, R3a is hydrogen, halogen, hydroxy, R16, -OR16, OCOR16, -OSO2R16, or tri(C1-C15 hydrocarbyl)silyloxy, R4 is hydrogen, halogen or R17, R5 is R5a or Z or together with R2 denotes an oxy group -O-, R5a is hydrogen, halogen, hydroxy, R18, -OR18, -OCOR18, -OSO2R18, or tri(C1-C15 hydrocarbyl)silyloxy, or together with R6 denotes a C1-C15 hydrocarbylidenedioxy group, R6 is halogen, hydroxy, -OR19, -OCOR19, -OSO2R19 or B1, or together with R5 denotes a C1-C15 hydrocarbylidenedioxy group, provided that R6 is not B1 when R1 is a group of formula (II) in which R14 is B2, R7 is hydrogen or R7a, R7a is R20, -COR20, -SO2R20 or tri(C1-C15 hydrocarbyl)silyl, or together with the attached oxygen atom and R0 denotes a C1-C15 hydrocarbylidenedioxy group, R8 is hydrogen, halogen, hydroxy, R21, -OR21, -OCOR21, -OSO2R21 or together with R10 denotes a valence bond, R9 is hydrogen, halogen or R22, R10 is hydrogen, halogen, hydroxy, R23, -OR23, -OCOR23 or -OSO2R23, or together with R8 denotes a valence bond, R11 is hydrogen, halogen or R24, R12 is hydrogen or R12a, or R12O- together with R13 denotes a C1-C15 hydrocarbylidenedioxy group, R12a is R25, -COR25, -SO2R25 or tri(C1-C15 hydrocarbyl)silyl, R13 is R13a or Z, R13a is hydrogen, halogen, hydroxy, R26, -OR26, -OCOR26, -OSO2R26 or tri(C1-C15 hydrocarbyl)silyloxy, or together with R14 denotes a C1-C15 hydrocarbylidenedioxy group, or together with R12O- denotes a C1-C15 hydrocarbylidenedioxy group, R14 is halogen, hydroxy, -OR27, -OCOR27, -OSO2R27, or B2 or together with R13 denoted a C1-C15 hydrocarbylidenedioxy group, provided that R14 is not B2 when R6 is B1, R15 is hydrogen or R15a, R15a is a C1 to C10 aliphatic group, a C3 to C8 cycloaliphatic group, a C6 to C15 aromatic group or a C7 t

Baxter, Anthony David
Taylor, roger john
Collingwood, Stephen Paul

JP50997096A

June 30, 1998

August 17, 1995

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Novartis Akchen Gezel Shaft

A61K31/70; A61K31/7024; A61K31/7042; A61K31/7048; A61K31/7052; A61K31/7064; A61K31/7068; A61K31/7072; A61K31/7076; A61K31/7135; A61P31/12; A61P35/00; A61P43/00; C07D405/04; C07F9/32; C07F19/00; C07H9/04; C07H13/02; C07H13/04; C07H13/06; C07H13/08; C07H19/01; C07H19/04; C07H19/06; C07H19/16; C07H21/00; C07H23/00; (IPC1-7): C07F9/32; A61K31/70; C07D405/04; C07F19/00; C07H9/04; C07H13/02; C07H13/06; C07H19/01; C07H19/06; C07H19/16; C07H23/00

Takashi Ishida (3 others)

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