CAS: 134678-17-4; 4-Amino-1-((2R,5S)-2-(Hydroxymethyl)-1,3-Oxathiolan-5-yl)Pyrimidin-2(1H)-One

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CAS号131086-21-0 拉米夫定 | CAS号147027-10-9 5-(4-氨基-2-氧代-2H... | CAS号69-72-7 水杨酸 | CAS号173522-96-8 水杨酸拉米呋啶 | CAS号145985-97-3 cis-2-[[(tert-b... | CAS号1091585-31-7 (2R,5S)-5-(4'-a... | CAS号173522-96-8 水杨酸拉米呋啶

4-Amino-1-[(2R,5S)-2-(Hydroxymethyl)-1,3-Oxathiolan-5-Yl]Pyrimidin-2-One;4-Nitrobenzoic Acid置于三乙胺体系中,用 乙醇 用作溶剂,以90%的收率获得拉米夫定
参考文献:A Process For Stereoselective Synthesis Of Lamivudine
标题:A Process For Stereoselective Synthesis Of Lamivudine

专利信息

专利号:US-7122693-B2
优先权日:1988-04-11
标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof
发明人：BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE
权利人:SHIRE BIOCHEM INC
摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.

专利号:US-8304540-B2
优先权日:2007-05-18
标题:Process for stereoselective synthesis of lamivudine
发明人：LI JINLIANG; LV FENG
权利人:LI JINLIANG; LV FENG; SHANGHAI DESANO PHARMACEUTICAL HOLDING CO LTD
摘要:The present invention discloses a process for stereoselective synthesis of Lamivudine comprising the following steps: (a) performing a glycosylation reaction between the compound of formula (I) and cytosine or protected cytosine, and separating the reaction product by recrystallization to obtain the intermediate of formula (II); and (b) deprotecting the intermediate of formula (II) to obtain Lamivudine.

专利号:US-6143748-A
优先权日:1995-03-31
标题:Process for synthesis of nucleoside analogues
发明人：SAMANO MIRNA C; SAMANO VICENTE; GOODYEAR MICHAEL DAVID
权利人:GLAXO WELLCOME INC
摘要:The present invention is concerned with a process for the preparation of antiviral 1,3-oxathiolane nucleosides comprising an intramolecular glycosylation reaction to produce exclusively the β-diastereomer, and intermediates useful in the process.

专利号:US-8748604-B2
优先权日:2010-03-04
标 题 :Process for stereoselective synthesis of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine
发明人：KSHIRSAGAR PRAKASH BHIMAJI; BHOGE SATISH MANOHAR; RICHHARIYA SANTOSH; SINGH KAPTAN
权利人:KSHIRSAGAR PRAKASH BHIMAJI; BHOGE SATISH MANOHAR; RICHHARIYA SANTOSH; SINGH KAPTAN; RANBAXY LAB LTD
摘要:The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof.

专利号:US-6329522-B1
优先权日:1994-04-23
标题:Process for the diastereoselective synthesis of nucleoside analogues
发明人：HILL MALCOLM LEITHEAD; WHITEHEAD ANDREW JONATHAN; HORNBY ROY; HALLETT PETER; GOODYEAR MICHAEL DAVID; DWYER P OWEN
权利人:GLAXO GROUP LTD
摘要:The invention relates to a diastereoselective process for the preparation of compounds of formula (1), wherein W is S, S=O, SO2 or O; X is S, S=O, SO2 or O; R1 is hydrogen or acyl, and R2 is a purine or pyrimidine base or an analogue or derivative thereof.

专利号:US-6927291-B2
优先权日:2001-03-01
标 题:Method for the synthesis of 2′,3′-dideoxy-2′,3′-didehydronucleosides
发明人：JIN FUQIANG; CONFALONE PASQUALE N
权利人:PHARMASSET LTD
摘要:An efficient synthetic route to antiviral 2′,3′-dideoxy-2′,3′-didehydro-nucleosides, such as 2′,3′-dideoxy and 2′- or 3′-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of β-D and β-L-2′,3′-dideoxy-2′,3′-didehydro-nucleosides is described that includes: activating a compound of structure (1) n n nwherein B is a pyrimidine or purine base and Y is O, S or CH 2 with an acyl halide of the formula X—C(â•?O)R 1 , X—C(â•?O)C(R 1 ) 2 OC(â•?O)R 1 or X—C(â•?O)OR 1 (wherein X is a halogen, and each R 1 is independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2′,3′-dideoxy-2′,3′-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2′-acyl-3′-halonucleoside, the 3′-acyl-2′-halonucleoside, or a mixture thereof.