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(2'R)-2'-脱氧-2'-氟-2'-甲基脲苷 | 863329-66-2

物质功能分类

医药中间体 - 原料药中间体

分子结构分类

有机化合物 - 核苷、核苷酸和类似物 - 嘧啶核苷

中文名称

(2'R)-2'-脱氧-2'-氟-2'-甲基脲苷

中文别名

(2R)-2-脱氧-2-氟-2-甲基-尿苷；2'-脱氧-2--氟-2'-C-甲基尿苷；(2'R)-2'-脱氧-2'-氟-2'-甲基尿苷

英文名称

2'-deoxy-2'-fluoro-2'-methyluridine

英文别名

1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyltetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione；(2'R)-2'-deoxy-2'-fluoro-2'-methyluridine；2'-deoxy-2'-fluoro-2'-C-methyluridine；1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydroxymethyl-3-methyltetrahydrofuran-2-yl)pyrimidine-2,4-dione；GS-331007；PSI-6206；1-[(2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidine-2,4-dione

CAS

863329-66-2

化学式

C₁₀H₁₃FN₂O₅

mdl

——

分子量

260.222

InChiKey

ARKKGZQTGXJVKW-VPCXQMTMSA-N

BEILSTEIN

——

EINECS

——

物化性质

熔点：

237-238℃
密度：

1.55
溶解度：

可溶于DMSO（轻微）、甲醇（轻微、加热）

计算性质

辛醇/水分配系数(LogP)：

-1.1
重原子数：

18
可旋转键数：

2
环数：

2.0
sp3杂化的碳原子比例：

0.6
拓扑面积：

99.1
氢给体数：

3
氢受体数：

6

安全信息

海关编码：

2934999090
危险性防范说明：

P261,P280,P305+P351+P338
危险性描述：

H302,H315,H319,H332,H335
储存条件：

温度低于0℃；请避免加热。

SDS

SDS：a0e68f8ad248422af19e85f87ac5b58f

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制备方法与用途

应用中的(2'R)-2'-脱氧-2'-氟-2'-甲基脲苷是一种关键的医药中间体，尤其在sfoSbuvir（CAS: 1190307-88-0）的生产中至关重要。该化合物具有重要的应用意义和经济价值。

2014年1月17日，丙型肝炎新药Sovaldi（sofosbuvir，400mg片剂）获欧盟批准，作为抗病毒治疗方案的一部分，用于慢性丙型肝炎（HCV）成人感染者的治疗。Sovaldi是一种每日一次的口服核苷类似物聚合酶抑制剂，此次批准为该药在整个欧盟的上市铺平了道路。在此之前，Sovaldi已于2013年11月获得了欧洲药品管理局（EMA）人用医药产品委员会（CHMP）的积极意见。在美国，Sovaldi于2013年12月获FDA批准，是首个获批用于慢性丙型肝炎全口服治疗方案的药物，在特定基因型患者的治疗中可消除对传统注射药物干扰素（IFN）的需求。

在欧洲和世界各地，慢性丙型肝炎（HCV）是导致肝癌和肝移植的主要原因之一。

生物活性方面，PSI-6206 (RO-2433, GS-331007) 是一种有效的HCV RNA依赖性RNA聚合酶抑制剂，靶向NS5B聚合酶。

用途包括sofosbuvir/1190307-88-0中间体的生产。

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
——	(2'R)-2'-deoxy-2'-fluoro-2'-methyluridine-3',5'-diacetate	——	C₁₄H₁₇FN₂O₇	344.297
4-氨基-1-((2R,3R,4R,5R)-3-氟-4-羟基-5-(羟基甲基)-3-甲基四氢呋喃-2-基)嘧啶-2(1H)-酮	(2'R)-2'-deoxy-2'-fluoro-2'-methylcytidine	817204-33-4	C₁₀H₁₄FN₃O₄	259.237
索氟布韦中间体 SF-C2	3',5'-di-O-benzoyl-2'-deoxy-2'-fluoro-2'-C-methyluridine	863329-65-1	C₂₄H₂₁FN₂O₇	468.438
2’-C-甲基尿苷	2'-C-methyluridine	31448-54-1	C₁₀H₁₄N₂O₆	258.231
——	1-(2'-C-methyl-β-D-arabinofuranosyl)uracil	114262-49-6	C₁₀H₁₄N₂O₆	258.231
(2'R)-N-苯甲酰基-2'-脱氧-2'-氟-2'-甲基胞苷 3',5'-二苯甲酸酯	(2'R)-N-benzoyl-2'-deoxy-2'-fluoro-2'-methylcytidine-3',5'-dibenzoate	817204-32-3	C₃₁H₂₆FN₃O₇	571.562
尿嘧啶核苷	uridine	58-96-8	C₉H₁₂N₂O₆	244.204
——	2′,3′,5′-tri-O-benzoyl-2′-C-methyluridine	23643-36-9	C₃₁H₂₆N₂O₉	570.555
——	3',5'-di-O-benzoyluridine	54618-11-0	C₂₃H₂₀N₂O₈	452.42
3',5'-O-(1,1,3,3-四异丙基-1,3-二硅氧烷)尿苷	3',5'-(1,1,3,3-tetraisopropyldisiloxane-1,3-diyl)uridine	69304-38-7	C₂₁H₃₈N₂O₇Si₂	486.713
——	1-((6aR,8R,9aS)-2,2,4,4-tetraisopropyl-9-methylenetetrahydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl)pyrimidine-2,4(1H,3H)-dione	102789-14-0	C₂₂H₃₈N₂O₆Si₂	482.725
3',5'-O-(四异丙基二硅氧烷-1,3-二基)-2'-氧代尿苷	1-((6aR,8R,9aR)-2,2,4,4-tetraisopropyl-9-oxotetrahydro-6H-furo[3,2-f][1,3,5,2,4]trioxadisilocin-8-yl)pyrimidine-2,4(1H,3H)-dione	84828-97-7	C₂₁H₃₆N₂O₇Si₂	484.697
——	(2R,3R,3aS,9aR)-3-hydroxy-2-(hydroxymethyl)-3a-methyl-2,3,3a,9a-tetrahydro-6H-furo[2',3':4,5]oxazolo[3,2-a]pyrimidin-6-one	944476-40-8	C₁₀H₁₂N₂O₅	240.216
2,2'-脱水尿苷	2,2'-Anhydrouridine	3736-77-4	C₉H₁₀N₂O₅	226.189

下游产品

中文名称	英文名称	CAS号	化学式	分子量
索非布韦杂质34	GS-606965	1015073-43-4	C₁₀H₁₄FN₂O₈P	340.202
——	2-cyanoethyl [(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methyl 3-hexadecoxypropyl phosphite	——	C₃₂H₅₅FN₃O₈P	659.776
——	[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methyl 3-hexadecoxypropyl hydrogen phosphate	——	C₂₉H₅₂FN₂O₉P	622.712
——	2-cyanoethyl [(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methyl 3-hexadecoxypropyl phosphate	——	C₃₂H₅₅FN₃O₉P	675.776
——	(2'R)-2'-deoxy-2'-fluoro-2'-methyluridine-3',5'-diacetate	——	C₁₄H₁₇FN₂O₇	344.297
——	1-((2R,3R,4S,5S)-3,5-difluoro-4-hydroxy-5-(hydroxymethyl)-3-methyl-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione	1443648-78-9	C₁₀H₁₂F₂N₂O₅	278.212
——	3′-O-tert-butyldimethylsilyl-2′-deoxy-2′-α-fluoro-2′-β-C-methyl uridine	1244762-86-4	C₁₆H₂₇FN₂O₅Si	374.485
——	β-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate	1015073-42-3	C₁₀H₁₆FN₂O₁₄P₃	500.162
——	benzyl (2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-2-(hydroxymethyl)-4-methyl-tetrahydrofuran-3-yl carbonate	1256490-58-0	C₁₈H₁₉FN₂O₇	394.356
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](ethoxy)phosphorylamino}propionic acid methyl ester	1250829-95-8	C₁₆H₂₅FN₃O₉P	453.361
——	5-bromo-1-((2R,3R,4S,5S)-3,5-difluoro-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidine-2,4-dione	1443648-79-0	C₁₀H₁₁BrF₂N₂O₅	357.109
——	9-[5′,6′-dideoxy-6′-(bispivaloyloxymethylphosphinyl)-2′-deoxy-2′-α-fluoro-2′-β-C-methyl-D-ribohexofuranosyl]uridine	1393526-65-2	C₂₃H₃₆FN₂O₁₁P	566.518
——	(2S,3R,4R,5R)-3-[tert-butyl(dimethyl)silyl]oxy-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-4-methyloxolane-2-carbaldehyde	1244762-90-0	C₁₆H₂₅FN₂O₅Si	372.469
——	1-[(2R,3R,4R,5R)-3-fluoro-4-[[hydroxy-di(propan-2-yl)silyl]oxy-di(propan-2-yl)silyl]oxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidine-2,4-dione	1256490-55-7	C₂₂H₄₁FN₂O₇Si₂	520.746
——	1-((2R,3R,4R)-3-fluoro-4-hydroxy-3-methyl-5-methylene-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione	1365257-02-8	C₁₀H₁₁FN₂O₄	242.207
——	{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}acetic acid methyl ester	1250829-96-9	C₁₉H₂₃FN₃O₉P	487.378
——	benzyl (2R,3R,4R,5R)-2-((tert-butyldimethylsilyloxy)methyl)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-4-methyl-tetrahydrofuran-3-yl carbonate	1315584-51-0	C₂₄H₃₃FN₂O₇Si	508.619
索非布韦杂质53	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}propionic acid methyl ester	1015255-46-5	C₂₀H₂₅FN₃O₉P	501.405
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}propionic acid ethyl ester	1064684-30-5	C₂₁H₂₇FN₃O₉P	515.432
——	sofosbuvir	1190307-88-0	C₂₂H₂₉FN₃O₉P	529.459
索非布韦R-磷酸盐	sofosbuvir	1190308-01-0	C₂₂H₂₉FN₃O₉P	529.459
索罗布维	sofosbuvir	1064684-44-1	C₂₂H₂₉FN₃O₉P	529.459
索非布韦杂质19	(R)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}propionic acid isopropyl ester	1064684-71-4	C₂₂H₂₉FN₃O₉P	529.459
——	((R)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-pyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyl-tetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)-D-alanine isopropyl ester	——	C₂₂H₂₉FN₃O₉P	529.459
——	sofosbuvir	1190307-88-0	C₂₂H₂₉FN₃O₉P	529.459
——	2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine 5'-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate	1365634-52-1	C₂₂H₂₉FN₃O₈PS	545.526
——	[[(2S,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-hydroxyphosphoryl] phosphono hydrogen phosphate	1613590-47-8	C₁₀H₁₅F₂N₂O₁₄P₃	518.152
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}propionic acid pentyl ester	1064684-58-7	C₂₄H₃₃FN₃O₉P	557.513
——	(S)-2-{(4-bromophenoxy)[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy]phosphorylamino}propionic acid methyl ester	1064684-25-8	C₂₀H₂₄BrFN₃O₉P	580.301
——	(S)-2-{(4-chlorophenoxy)[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy]phosphorylamino}propionic acid ethyl ester	1064684-61-2	C₂₁H₂₆ClFN₃O₉P	549.877
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}butyric acid methyl ester	1064684-64-5	C₂₁H₂₇FN₃O₉P	515.432
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](4-fluorophenoxy)phosphorylamino}propionic acid ethyl ester	1064684-46-3	C₂₁H₂₆F₂N₃O₉P	533.423
——	(S)-2-{(4-chlorophenoxy)[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy]phosphorylamino}propionic acid isopropyl ester	1250830-04-6	C₂₂H₂₈ClFN₃O₉P	563.904
——	(S)-2-{(4-bromophenoxy)[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy]phosphorylamino}propionic acid ethyl ester	1250830-03-5	C₂₁H₂₆BrFN₃O₉P	594.328
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}-3-methylbutyric acid methyl ester	1064684-23-6	C₂₂H₂₉FN₃O₉P	529.459
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}propionic acid phenyl ester	1250829-93-6	C₂₅H₂₇FN₃O₉P	563.476
——	(S)-2-{(4-bromophenoxy)[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy]phosphorylamino}propionic acid isopropyl ester	1064684-74-7	C₂₂H₂₈BrFN₃O₉P	608.355
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}propionic acid cyclohexyl ester	1250829-92-5	C₂₅H₃₃FN₃O₉P	569.524
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}-4-methylpentanoic acid methyl ester	1250829-97-0	C₂₃H₃₁FN₃O₉P	543.486
索菲布韦杂质	[(2S,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-2,4-difluoro-2-(hydroxymethyl)-4-methyloxolan-3-yl] benzoate	1613589-57-3	C₁₇H₁₆F₂N₂O₆	382.321
——	(2S)-2-((([1,1'-biphenyl]-4-yloxy)(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)phosphoryl)amino)propanoic acid isopropyl ester	——	C₂₈H₃₃FN₃O₉P	605.557
——	(S)-2-[[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](naphthalen-1-yloxy)phosphorylamino]propionic acid methyl ester	1250829-94-7	C₂₄H₂₇FN₃O₉P	551.465
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}-4-methylsulfanylbutyric acid methyl ester	1250829-98-1	C₂₂H₂₉FN₃O₉PS	561.525
——	[1,1,1,3,3,3‐D₆]propan‐2‐yl ((S)‐(((2R,3R,4R,5R)‐5‐(2,4‐dioxo‐3,4‐dihydropyrimidin‐1(2H)‐yl)‐4‐fluoro‐3‐hydroxy‐4‐methyltetrahydrofuran‐2‐yl)methoxy)(phenoxy)phosphoryl)‐L‐alaninate	——	C₂₂H₂₉FN₃O₉P	535.411
——	[(2S,3S,4R,5R)-3-benzoyloxy-5-(2,4-dioxopyrimidin-1-yl)-2,4-difluoro-4-methyloxolan-2-yl]methyl benzoate	1443648-77-8	C₂₄H₂₀F₂N₂O₇	486.429
——	(S)-2-{[(2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-ylmethoxy](phenoxy)phosphorylamino}propionic acid 4-fluorobenzyl ester	1064684-66-7	C₂₆H₂₈F₂N₃O₉P	595.494
——	9-[5′,6′-vinyl-6′-(bispivaloyloxymethylphosphinyl)-2′-deoxy-2′-α-fluoro-2′-β-C-methyl-D-ribohexofuranosyl]uridine	1393526-41-4	C₂₉H₄₈FN₂O₁₁PSi	678.765
——	(2S)-2-((((3'-(N-methylcarbamoyl)-[1,1'-biphenyl]-4-yl)oxy)(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)phosphoryl)amino)propanoic acid isopropyl ester	——	C₃₀H₃₆FN₄O₁₀P	662.609
——	ethyl (2S)-2-[[[(2R,3R,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-4-fluoro-4-methyl-3-phenylmethoxycarbonyloxyoxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate	1315584-52-1	C₂₉H₃₃FN₃O₁₁P	649.567
——	(S)-2-{[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-phenoxy-phosphorylamino}-propionic acid isopropyl ester	1443648-59-6	C₂₂H₂₈F₂N₃O₉P	547.45
——	(S)-2-{(S)-[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-phenoxy-phosphorylamino}-propionic acid isopropyl ester	1443648-68-7	C₂₂H₂₈F₂N₃O₉P	547.45
——	(S)-2-{(R)-[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-phenoxy-phosphorylamino}-propionic acid isopropyl ester	1443648-69-8	C₂₂H₂₈F₂N₃O₉P	547.45
——	(S)-2-[[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-2-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-61-0	C₂₆H₃₀F₂N₃O₉P	597.509
——	(S)-2-[(S)-[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-2-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-64-3	C₂₆H₃₀F₂N₃O₉P	597.509
——	(S)-2-[(R)-[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-2-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-65-4	C₂₆H₃₀F₂N₃O₉P	597.509
——	[(2S,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3-benzoyloxy-2,4-difluoro-4-methyloxolan-2-yl]methyl benzoate	1613589-58-4	C₂₄H₂₁F₂N₃O₆	485.444
——	(S)-2-[(R)-[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-1-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-66-5	C₂₆H₃₀F₂N₃O₉P	597.509
——	(S)-2-[(S)-[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-1-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-67-6	C₂₆H₃₀F₂N₃O₉P	597.509
——	(S)-2-[[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-1-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-60-9	C₂₆H₃₀F₂N₃O₉P	597.509
——	(S)-2-[[(2S,3S,4R,5R)-5-(5-bromo-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-2-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-74-5	C₂₆H₂₉BrF₂N₃O₉P	676.406
——	(S)-2-[(S)-[(2S,3S,4R,5R)-5-(5-bromo-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-2-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-71-2	C₂₆H₂₉BrF₂N₃O₉P	676.406
——	(S)-2-[(R)-[(2S,3S,4R,5R)-5-(5-bromo-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-2-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-73-4	C₂₆H₂₉BrF₂N₃O₉P	676.406
——	(S)-2-[(S)-[(2S,3S,4R,5R)-5-(5-bromo-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-1-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-70-1	C₂₆H₂₉BrF₂N₃O₉P	676.406
——	(S)-2-[(R)-[(2S,3S,4R,5R)-5-(5-bromo-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-3-hydroxy-4-methyl-tetrahydro-furan-2-ylmethoxy]-(naphthalen-1-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-72-3	C₂₆H₂₉BrF₂N₃O₉P	676.406
——	(2S)-2-(((S)-((4-fluoro-1,2-dimethyl-1H-indol-5-yl)oxy)(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2-yl)methoxy)phosphoryl)amino)propanoic acid isopropyl ester	——	C₂₆H₃₃F₂N₄O₉P	614.54
——	(S)-2-[[(2S,3S,4R,5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-2,4-difluoro-4-methyl-3-propionyloxy-tetrahydro-furan-2-ylmethoxy]-(naphthalen-1-yloxy)-phosphorylamino]-propionic acid isopropyl ester	1443648-63-2	C₂₉H₃₄F₂N₃O₁₀P	653.574

反应信息

作为反应物：

描述：

(2'R)-2'-脱氧-2'-氟-2'-甲基脲苷在 N-甲基咪唑、盐酸作用下，以二氯甲烷、异丙醚、水为溶剂，反应 78.5h，生成 sofosbuvir

参考文献：

名称：

[EN] METHODS FOR TREATING HCV
[FR] PROCÉDÉS PERMETTANT DE TRAITER LE VIRUS DE L'HÉPATITE C (HCV)

摘要：

公开号：

WO2013040492A3
作为产物：

描述：

4-氨基-1-((2R,3R,4R,5R)-3-氟-4-羟基-5-(羟基甲基)-3-甲基四氢呋喃-2-基)嘧啶-2(1H)-酮在吡啶、甲醇、氨、溶剂黄146 作用下，以水为溶剂，反应 1.67h，生成 (2'R)-2'-脱氧-2'-氟-2'-甲基脲苷

参考文献：

名称：

NUCLEOSIDE PHOSPHORAMIDATE PRODRUGS

摘要：

本文披露了用于治疗哺乳动物病毒感染的核苷类衍生物的磷酰胺酯前药，该前药是一种化合物，其立体异构体、盐（酸性或碱性加合盐）、水合物、溶剂合物或结晶形式，由以下结构表示：同时还披露了治疗方法、用途和制备过程，每种方法均利用由式I表示的化合物。

公开号：

US20100016251A1

点击查看最新优质反应信息

文献信息

Azido nucleosides and nucleotide analogs

申请人：Alios BioPharma, Inc.

公开号：US09346848B2

公开（公告）日：2016-05-24

Disclosed herein are 4′-azido-substituted nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of 4′-azido-substituted nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a 4′-azido-substituted nucleoside, a nucleotide and/or an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.

本文披露了4'-偶氮基取代核苷、核苷酸及其类似物，包括其中一个或多个4'-偶氮基取代核苷、核苷酸及其类似物的药物组合物，以及它们的合成方法。本文还披露了使用4'-偶氮基取代核苷、核苷酸和/或其类似物来改善和/或治疗疾病和/或病况的方法，包括由副粘病毒和/或正粘病毒引起的感染。病毒感染的例子包括呼吸道合胞病毒（RSV）和流感感染。
SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF

申请人：Alios BioPharma, Inc.

公开号：US20150105341A1

公开（公告）日：2015-04-16

Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.

本文披露了核苷、核苷酸和核苷酸类似物，以及它们的合成方法以及利用一个或多个核苷、核苷酸和核苷酸类似物治疗如小核糖核病毒和/或黄病毒科感染等疾病和/或症状的方法。
[EN] NUCLEOTIDE AND NUCLEOSIDE COMPOSITIONS AND USES RELATED THERETO<br/>[FR] COMPOSITIONS À BASE DE NUCLÉOTIDE ET DE NUCLÉOSIDE ET UTILISATIONS CORRESPONDANTES

申请人：UNIV EMORY

公开号：WO2015038596A1

公开（公告）日：2015-03-19

This disclosure relates to nucleotide and nucleoside therapeutic compositions and uses in treating infectious diseases, viral infections, and cancer, where the base of the nucleotide or nucleoside contains at least one thiol, thione or thioether.

这份披露涉及到核苷酸和核苷类治疗组合物，用于治疗传染病、病毒感染和癌症，在这些组合物中，核苷酸或核苷的碱基至少含有一个硫醇、硫酮或硫醚。
[EN] PROCESS FOR THE PREPARATION OF (Sp)-SOFOSBUVIR AND INTERMEDIATES THEREOF<br/>[FR] PROCÉDÉ DE PRÉPARATION DU (SP)-SOFOSBUVIR ET DE SES INTERMÉDIAIRES

申请人：ALEMBIC PHARMACEUTICALS LTD

公开号：WO2018025195A1

公开（公告）日：2018-02-08

The present invention is directed towards process for preparation of an optically pure (Sp)-Sofosbuvir of Formula-(I) and its intermediate namely (Sp)-isomer of isopropyl alanyl phosphoramidate of Formula (III) thereof.

本发明涉及一种制备光学纯(Sp)-索非布韦（化学式(I)）及其中间体即异丙基丙氨基磷酰胺的(Sp)-异构体（化学式(III)）的方法。
一种呋喃核糖磷酸酯衍生物的制备方法

申请人：南通常佑药业科技有限公司

公开号：CN104610404B

公开（公告）日：2016-04-06

本发明公开了一种呋喃核糖磷酸酯衍生物的制备方法，其制备步骤包括：以L-丙氨酸异丙酯盐酸盐、苯酚二氯磷酸酯和取代苯酚为起始原料，在碱的作用下进行对接反应；(2R)-2-脱氧-2-氟-2-甲基-D-赤式戊糖酸？GAMMA-内酯？3,5-二苯甲酸酯在二氯甲烷或醚类溶剂中经强还原剂作用将羰基还原为醇羟基；中间体式2-1在碱作用下，与对甲苯磺酰氯反应得到对甲苯磺酸酯；中间体式2-2与苯甲酰胞嘧啶衍生物在缩合剂作用下进行对接反应；中间体式2-3在有机酸作用下将胞嘧啶转化为尿嘧啶；中间体式2-4在碱试剂作用下脱去苯甲酰保护；中间体式2-5与式1在格式试剂作用下对接得到Sofosbuvir。