N-乙酰基-3',5'-O-[1,1,3,3-四(异丙基)-1,3-二硅氧烷二基]胞苷 - CAS号 85335-73-5

物化性质

密度：

1.24±0.1 g/cm3(Predicted)

计算性质

辛醇/水分配系数(LogP)：

3.42
重原子数：

35
可旋转键数：

6
环数：

3.0
sp3杂化的碳原子比例：

0.78
拓扑面积：

119
氢给体数：

2
氢受体数：

7

安全信息

危险性防范说明：

P261,P305+P351+P338
危险性描述：

H302,H315,H319,H335
储存条件：

存储条件：2-8℃，请保持干燥。

SDS

SDS：3e42427939bc42df389d7c8771468dbd

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上下游信息

上游原料

中文名称	英文名称	CAS号	化学式	分子量
(+)-3’,5’-O-(1,1,3,3-四异丙基-1,3-二硅氧烷)胞苷	3',5'-O-[(1,1,3,3-tetraisopropyl)-1,3-disiloxanediyl]cytidine	69304-42-3	C₂₁H₃₉N₃O₆Si₂	485.728
N-乙酰胞嘧啶核苷	N-acetylcytidine	3768-18-1	C₁₁H₁₅N₃O₆	285.257
胞苷	CYTIDINE	65-46-3	C₉H₁₃N₃O₅	243.219
尿嘧啶核苷	uridine	58-96-8	C₉H₁₂N₂O₆	244.204

下游产品

中文名称	英文名称	CAS号	化学式	分子量
——	N-[1-[(6aR,8R,9R,9aR)-9-methoxy-2,2,4,4-tetra(propan-2-yl)-6a,8,9,9a-tetrahydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	199593-14-1	C₂₄H₄₃N₃O₇Si₂	541.792
——	CEM C-1	877774-40-8	C₂₇H₄₆N₄O₈Si₂	610.855
——	N(4)-acetyl-3',5'-O-(1,1,3,3-tetraisopropyldisiloxane-1,3-diyl)-2'-O-(methylthiomethyl)cytidine	201667-26-7	C₂₅H₄₅N₃O₇SSi₂	587.885
(+)-3’,5’-O-(1,1,3,3-四异丙基-1,3-二硅氧烷)胞苷	3',5'-O-[(1,1,3,3-tetraisopropyl)-1,3-disiloxanediyl]cytidine	69304-42-3	C₂₁H₃₉N₃O₆Si₂	485.728
——	N-(1-{(2R,3R,3aR,9aR)-3-[1-(2-Cyano-ethoxy)-ethoxy]-5,5,7,7-tetraisopropyl-tetrahydro-1,4,6,8-tetraoxa-5,7-disila-cyclopentacycloocten-2-yl}-2-oxo-1,2-dihydro-pyrimidin-4-yl)-acetamide	828247-67-2	C₂₈H₄₈N₄O₈Si₂	624.882
——	N-[1-[(6aR,8R,9aS)-9-methylidene-2,2,4,4-tetra(propan-2-yl)-6a,9a-dihydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	170112-37-5	C₂₄H₄₁N₃O₆Si₂	523.777
——	N⁴-acetyl-1-<3,5-O-(tetraisopropyldisiloxane-1,3-diyl)-β-D-erythro-pentofuran-2-ulosyl>cytosine	140859-16-1	C₂₃H₃₉N₃O₇Si₂	525.75
——	N-[1-[(6aR,8R,9R,9aS)-9-cyano-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403250-61-2	C₂₅H₄₂N₄O₆Si₂	550.803
——	N-[1-[(2R,3R,4S,5R)-3-cyano-4-[[hydroxy-di(propan-2-yl)silyl]oxy-di(propan-2-yl)silyl]oxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]-2-oxopyrimidin-4-yl]acetamide	1491025-66-1	C₂₅H₄₄N₄O₇Si₂	568.818
——	N-[1-[(6aR,8R,9R,9aR)-9-methyl-9-methylsulfanyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-55-7	C₂₅H₄₅N₃O₆SSi₂	571.886
——	(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-[[hydroxy-di(propan-2-yl)silyl]oxy-di(propan-2-yl)silyl]oxy-5-(hydroxymethyl)-3-methyloxolane-3-carbonitrile	1491025-69-4	C₂₃H₄₂N₄O₆Si₂	526.781
——	N-[1-[(6aR,8R,9R,9aS)-9-azido-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-53-5	C₂₄H₄₂N₆O₆Si₂	566.805
N-乙酰基-2'-O-甲基胞苷	N⁴-acetyl-2'-O-methyl cytidine	113886-71-8	C₁₂H₁₇N₃O₆	299.283
——	1-[(6aR,8R,9R,9aR)-9-chloro-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-4-aminopyrimidin-2-one	1403249-59-1	C₂₂H₄₀ClN₃O₅Si₂	518.201
——	1-[(6aR,8R,9R,9aS)-9-amino-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-4-aminopyrimidin-2-one	1403249-67-1	C₂₂H₄₂N₄O₅Si₂	498.77
——	1-[(6aR,8R,9R,9aS)-9-azido-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-4-aminopyrimidin-2-one	1403249-66-0	C₂₂H₄₀N₆O₅Si₂	524.768
——	N-[1-[(6aR,8R,9R,9aR)-9-methyl-9-methylsulfonyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-62-6	C₂₅H₄₅N₃O₈SSi₂	603.885
——	N-[1-[(6aR,8R,9R,9aS)-9-methyl-2,2,4,4-tetra(propan-2-yl)-9-(triazol-1-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl]-2-oxopyrimidin-4-yl]acetamide	1403249-64-8	C₂₆H₄₄N₆O₆Si₂	592.843
——	N-[(6aR,8R,9R,9aS)-8-(4-amino-2-oxopyrimidin-1-yl)-9-methyl-2,2,4,4-tetra(propan-2-yl)-6,6a,8,9a-tetrahydrofuro[3,2-f][1,3,5,2,4]trioxadisilocin-9-yl]acetamide	1403249-68-2	C₂₄H₄₄N₄O₆Si₂	540.808
N-(1-((2r,3r,4r,5r)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-4-羟基-3-甲氧基四氢呋喃-2-基)-2-氧代-1,2-二氢嘧啶-4-基)乙酰胺	N-(1-((2R,3R,4R,5R)-5-((bis(4-Methoxyphenyl)(phenyl)methoxy)methyl)-4-hydroxy-3-methoxytetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)acetamide	199593-08-3	C₃₃H₃₅N₃O₈	601.656
——	2-methylpropyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-[[hydroxy-di(propan-2-yl)silyl]oxy-di(propan-2-yl)silyl]oxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1491026-66-4	C₃₆H₆₀N₅O₁₀PSi₂	810.045
——	N-(1-{(2R,3R,4R,5R)-5-[Bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-3-[1-(2-cyano-ethoxy)-ethoxy]-4-hydroxy-tetrahydro-furan-2-yl}-2-oxo-1,2-dihydro-pyrimidin-4-yl)-acetamide	828247-75-2	C₃₇H₄₀N₄O₉	684.746
N-乙酰基-5’-O-(4,4-二甲氧基三苯甲基)-2’-O-甲基胞苷-3’-(2-氰基乙基-N,N-二异丙基)亚磷酰胺	2'-OMe-Ac-C Phosphoramidite	199593-09-4	C₄₂H₅₂N₅O₉P	801.877
——	Diisopropyl-phosphoramidous acid (2R,3R,4R,5R)-5-(4-acetylamino-2-oxo-2H-pyrimidin-1-yl)-2-[bis-(4-methoxy-phenyl)-phenyl-methoxymethyl]-4-[1-(2-cyano-ethoxy)-ethoxy]-tetrahydro-furan-3-yl ester 2-cyano-ethyl ester	828247-88-7	C₄₆H₅₇N₆O₁₀P	884.967
——	N-[1-[(2R,3R,4S,5R)-3-cyano-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]-2-oxopyrimidin-4-yl]acetamide	1491021-51-2	C₁₃H₁₆N₄O₅	308.294
——	2'-O-(1,1-dioxo-1λ6-thiomorpholine-4-carbothioate)-5'-O-(4,4'-dimethoxytrityl)-N2-acetylcytidine-3'-O-(β-cyanoethyl)-N,N-diisopropylphosphoramidite	1219089-87-8	C₄₆H₅₇N₆O₁₁PS₂	965.098
——	N-[1-[(2R,3R,4S,5R)-3-azido-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]-2-oxopyrimidin-4-yl]acetamide	1403567-97-4	C₁₂H₁₆N₆O₅	324.296
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-4-azido-3-hydroxy-4-methyl-5-[4-(2-methylpropanoylamino)-2-oxopyrimidin-1-yl]oxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1605283-90-6	C₂₆H₃₆N₇O₉P	621.587
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-4-cyano-3-hydroxy-4-methyl-5-[2-oxo-4-(2-propylpentanoylamino)pyrimidin-1-yl]oxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1605283-80-4	C₃₁H₄₄N₅O₉P	661.692
——	[(2R,3S,4R,5R)-4-cyano-4-methyl-5-[4-(2-methylpropanoylamino)-2-oxopyrimidin-1-yl]-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-methylpropanoate	1605283-84-8	C₃₁H₄₂N₅O₁₀P	675.676
——	[(2R,3S,4R,5R)-4-azido-4-methyl-5-[4-(2-methylpropanoylamino)-2-oxopyrimidin-1-yl]-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-methylpropanoate	1605283-89-3	C₃₀H₄₂N₇O₁₀P	691.678
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403574-71-9	C₂₂H₃₀N₇O₈P	551.496
——	methyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxy-4-methyl-4-(triazol-1-yl)oxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403249-80-8	C₂₂H₂₈N₇O₈P	549.48
——	methyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403568-00-2	C₂₀H₂₆N₇O₈P	523.442
——	propan-2-yl (2S)-2-[[[(2R,3S,4R,5R)-4-amino-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403250-92-9	C₂₂H₃₂N₅O₈P	525.499
——	[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-4-methyl-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-methylpropanoate	1605283-86-0	C₂₆H₃₆N₇O₉P	621.587
——	1-[(4aR,6R,7R,7aS)-7-azido-7-methyl-2-oxo-2-propan-2-yloxy-4,4a,6,7a-tetrahydrofuro[3,2-d][1,3,2]dioxaphosphinin-6-yl]-4-aminopyrimidin-2-one	1403250-40-7	C₁₃H₁₉N₆O₆P	386.304
——	4-amino-1-[(2R,3R,4S,5R)-3-azido-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidin-2-one	1403249-54-6	C₁₀H₁₄N₆O₄	282.259
——	methyl (2S)-2-[[[(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxy-4-methyl-4-methylsulfanyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1403249-81-9	C₂₁H₂₉N₄O₈PS	528.523
——	butyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-hydroxy-4-methyloxolan-2-yl]methoxy-naphthalen-1-yloxyphosphoryl]amino]propanoate	1491021-88-5	C₂₈H₃₄N₅O₈P	599.58
——	2-methylpropyl (2S)-2-[[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1491026-71-1	C₂₄H₃₂N₅O₈P	549.521
——	4-amino-1-[(2R,3R,4R,5R)-4-hydroxy-5-(hydroxymethyl)-3-methyl-3-methylsulfonyloxolan-2-yl]pyrimidin-2-one	1403249-63-7	C₁₁H₁₇N₃O₆S	319.338
——	4-amino-1-[(2R,3R,4R,5R)-4-hydroxy-5-(hydroxymethyl)-3-methyl-3-methylsulfanyloxolan-2-yl]pyrimidin-2-one	1403249-56-8	C₁₁H₁₇N₃O₄S	287.34
——	[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-azido-3-hydroxy-4-methyloxolan-2-yl]methyl (2-chlorophenyl) propan-2-yl phosphate	1403250-39-4	C₁₉H₂₄ClN₆O₇P	514.862
——	4-amino-1-[(2R,3R,4S,5R)-3-amino-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidin-2-one	1403249-61-5	C₁₀H₁₆N₄O₄	256.261
——	N-[(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-3-yl]acetamide	1403249-69-3	C₁₂H₁₈N₄O₅	298.299
——	4-amino-1-[(2R,3R,4S,5R)-4-hydroxy-5-(hydroxymethyl)-3-methyl-3-(triazol-1-yl)oxolan-2-yl]pyrimidin-2-one	1403249-65-9	C₁₂H₁₆N₆O₄	308.297
——	[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-4-methyl-2-[[[[(2S)-1-oxo-1-propan-2-yloxypropan-2-yl]amino]-phenoxyphosphoryl]oxymethyl]oxolan-3-yl] 2-propylpentanoate	1605283-78-0	C₃₁H₄₄N₅O₉P	661.692
——	1-[(4aR,6R,7R,7aS)-7-amino-7-methyl-2-oxo-2-propan-2-yloxy-4,4a,6,7a-tetrahydrofuro[3,2-d][1,3,2]dioxaphosphinin-6-yl]-4-aminopyrimidin-2-one	1403250-41-8	C₁₃H₂₁N₄O₆P	360.307
——	(4aR,6R,7R,7aS)-6-(4-amino-2-oxopyrimidin-1-yl)-7-methyl-2-propan-2-yloxy-4,4a,6,7a-tetrahydrofuro[3,2-d][1,3,2]dioxaphosphinine-7-carbonitrile	1491023-16-5	C₁₄H₁₉N₄O₅P	354.302
——	[[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-cyano-3-hydroxy-4-methyloxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	1491023-69-8	C₁₁H₁₇N₄O₁₃P₃	506.196
——	(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)-3-methyloxolane-3-carbonitrile	1491021-53-4	C₁₁H₁₄N₄O₄	266.257
——	(2R,3R,4S,5R)-2-(4-amino-2-oxopyrimidin-1-yl)-4-hydroxy-5-(hydroxymethyl)-3-methyloxolane-3-carboxamide	1403250-62-3	C₁₁H₁₆N₄O₅	284.272
2'-脱氧胞嘧啶核苷	2'-Deoxycytidine	951-77-9	C₉H₁₃N₃O₄	227.22

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反应信息

作为反应物：

描述：

N-乙酰基-3',5'-O-[1,1,3,3-四(异丙基)-1,3-二硅氧烷二基]胞苷在吡啶、四丁基氟化铵、 silver(l) oxide 作用下，以四氢呋喃、苯为溶剂，生成 N-(1-((2r,3r,4r,5r)-5-((双(4-甲氧基苯基)(苯基)甲氧基)甲基)-4-羟基-3-甲氧基四氢呋喃-2-基)-2-氧代-1,2-二氢嘧啶-4-基)乙酰胺

参考文献：

名称：

Ultrafast Cleavage and Deprotection of Oligonucleotides Synthesis and Use of C^AcDerivatives

摘要：

We have investigated the use of alkylamines as fast cleavage and deprotection reagents for the solid phase synthesis of oligonucleotides and found methylamine/ammonium hydroxide (or methylamine) as an efficient reagent. The transamination side product formed with the commonly used dC(bz) has been eliminated by the use of dC(Ac) phosphoramidite. This system has successfully been used in the synthesis of oligonucleotides and oligonucleoside phosphorothioates. DMT dC(Ac) hydrogen phosphonate and DMT ribo C-Ac-2'-OMe phosphoramidite also have been prepared and used in the synthesis of oligonucleotides.

DOI：

10.1080/07328319708006236
作为产物：

描述：

胞苷在吡啶作用下，以乙醇为溶剂，反应 18.25h，生成 N-乙酰基-3',5'-O-[1,1,3,3-四(异丙基)-1,3-二硅氧烷二基]胞苷

参考文献：

名称：

2'-CYANO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF USEFUL FOR THE TREATMENT OF VIRAL DISEASES

摘要：

本发明涉及式(I)的2'-氰基取代核苷衍生物及其药学上可接受的盐，其中B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-氰基取代核苷衍生物的组合物，以及使用这些2'-氰基取代核苷衍生物治疗或预防患者HCV感染的方法。

公开号：

US20140161770A1

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文献信息

[EN] 2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES<br/>[FR] DÉRIVÉS DE NUCLÉOSIDE 2'-SUBSTITUÉS ET PROCÉDÉS D'UTILISATION DE CEUX-CI POUR LE TRAITEMENT DE MALADIES VIRALES

申请人：MERCK SHARP & DOHME

公开号：WO2012142085A1

公开（公告）日：2012-10-18

The present invention relates to 2'-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2'-Substituted Nucleoside Derivative, and methods of using the 2'-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

本发明涉及式(I)的2'-取代核苷衍生物及其药学上可接受的盐，其中A、B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-取代核苷衍生物的组合物，以及使用这些2'-取代核苷衍生物治疗或预防患者HCV感染的方法。
2'-AZIDO SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES

申请人：Girijavallabhan Vinay

公开号：US20140206640A1

公开（公告）日：2014-07-24

The present invention relates to 2′-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R 1 , R 2 and R 3 are as defined herein. The present invention also relates to compositions comprising at least one 2′-Azido Substituted Nucleoside Derivative, and methods of using the 2′-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

本发明涉及式(I)的2'-叠氮基取代核苷衍生物及其药学上可接受的盐，其中B、X、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-叠氮基取代核苷衍生物的组合物，以及使用这些2'-叠氮基取代核苷衍生物治疗或预防患者HCV感染的方法。
[EN] 2'-METHYL SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES<br/>[FR] DÉRIVÉS DE NUCLÉOSIDES 2'-MÉTHYLE SUBSTITUÉS ET LEURS PROCÉDÉS D'UTILISATION DANS LE TRAITEMENT DE MALADIES VIRALES

申请人：MERCK SHARP & DOHME

公开号：WO2014062596A1

公开（公告）日：2014-04-24

The present invention relates to 2'-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2'-Methyl Substituted Nucleoside Derivative, and methods of using the 2'-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.

本发明涉及式(I)的2'-甲基取代核苷衍生物及其药学上可接受的盐，其中R、R1、R2和R3如本文所定义。本发明还涉及包含至少一种2'-甲基取代核苷衍生物的组合物，以及使用这些2'-甲基取代核苷衍生物治疗或预防患者HCV感染的方法。
[EN] PREPARATION OF INTERMEDIATES USEFUL IN THE SYNTHEIS OF 2'-CYANO-2'-DEOXY-N4-PALMITOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE<br/>[FR] PRÉPARATION D'INTERMÉDIAIRES UTILES DANS LA SYNTHÈSE DE 2'-CYANO-2'-DÉSOXY-N4-PALMITOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE

申请人：CYCLACEL LTD

公开号：WO2009136158A1

公开（公告）日：2009-11-12

The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2'; (ii) converting said compound of formula 682-2' into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2'-cyano-2'-deoxy-N4 -palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.

本发明涉及一种制备式682-4化合物的方法，该方法包括以下步骤：(i)将式682-1化合物转化为式682-2'化合物；(ii)将所述式682-2'化合物转化为式682-3化合物；以及(iii)将所述式682-3化合物转化为式682-4化合物。该发明的进一步方面涉及上述方法在制备2'-氰基-2'-脱氧-N4-棕榈酰-1-β-D-阿拉伯莫呋核苷的用途，这是一种嘧啶核苷，对治疗和/或预防癌症具有治疗作用。
[EN] INTERMEDIATE AND PROCESSES INVOLVED IN THE PREPARATION OF 2 ' -CYANO-2 ' -DE0XY-N4-PALMIT0YL-1-BETA-ARABIN0FURAN0SYLCYTOSINE<br/>[FR] INTERMÉDIAIRE ET PROCÉDÉS ASSOCIÉS À LA PRÉPARATION DE 2'-CYANO-2'-DÉSOXY-N4-PALMITOYL-1-BÊTA-ARABINOFURANOSYLCYTOSINE

申请人：CYCLACEL LTD

公开号：WO2009136162A1

公开（公告）日：2009-11-12

The present invention relates to a process for preparing a compound of formula (682-6'), said process comprising the steps of: formula (682-4), (682-5), (682-6'): (i) converting a compound of formula (682-4) into a compound of formula (682-5); and (ii) converting said compound of formula (682-5) into a compound of formula (682- 6'). Further aspects of the invention relate to the use of the above process in the preparation of 2'-cyano-2'-deoxy-N4-palmitoyl-l-β-D-arabinofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.

本发明涉及一种制备式（682-6'）化合物的方法，该方法包括以下步骤：式（682-4）、（682-5）、（682-6'）：（i）将式（682-4）化合物转化为式（682-5）化合物；以及（ii）将所述式（682-5）化合物转化为式（682-6'）化合物。该发明的进一步方面涉及上述方法在制备2'-氰基-2'-脱氧-N4-棕榈酰-1-β-D-阿拉伯呋喃核苷胞嘧啶中的应用，该核苷是治疗和/或预防癌症中具有治疗作用的。

N-乙酰基-3',5'-O-[1,1,3,3-四(异丙基)-1,3-二硅氧烷二基]胞苷 | 85335-73-5

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