CAS: 16251-45-9; (4S,5R)-4-Methyl-5-Phenyloxazolidin-2-One

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77943-39-6 875444-08-9 17097-67-5

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CAS号492-41-1 去甲麻黄碱 | CAS号503-38-8 氯甲酸三氯甲酯 | CAS号32315-10-9 三光气 | CAS号113322-99-9 tert-butyl (1R,... | CAS号75-08-1 乙硫醇 | CAS号79297-23-7 (1R,2S)-2-[(eth... | CAS号6638-79-5 二甲羟胺盐酸盐

(4S,5R)-4-Methyl-5-Phenyl-3-Propionyloxazolidin-2-One置于三氟甲磺酸二丁硼,三甲基铝,N,N-二异丙基乙胺体系中,用 四氢呋喃,乙醚,甲苯 用作溶剂,化学反应 3.5H,反应生成(4S,5R)-(-)-4-甲基-5-苯基-2-恶唑啉酮
参考文献:Aurilide,一种来自海兔dolabella Auricularia的细胞毒性二肽:分离,结构确定,合成和生物学活性
标题:Aurilide,一种来自海兔dolabella Auricularia的细胞毒性二肽:分离,结构确定,合成和生物学活性
摘要:对日本海兔dollabella Auricularia的细胞毒性成分进行生物测定指导的分馏,导致分离出26个成员的环二肽aurilide(1).通过包括2D NMR技术的光谱分析来确定1的总体结构.通过对1的酸水解产物进行手性HPLC分析并通过对映选择性合成由二羟基化脂肪酸部分产生的降解产物来确定绝对立体结构.的对映选择性合成1在12%的总收率(16步)来实现,并确认的绝对立体结构1.1的细胞毒性使用合成样品评估细胞毒性,发现合成样品对hela S 3细胞表现出强大的细胞毒性,Ic 50为0.011μg/ Ml.的进一步的生物学和药理学研究1已经通过使用合成的进行1.
Doi:10.1016/j.Tet.2004.06.125

专利信息

专利号:US-5554788-A
优先权日:1992-10-01
标 题 :Process for the stereoselective synthesis of 3-substituted 2-thiomethylpropionic acids
发明人：HOLLA WOLFGANG; KAMMERMEIER BERNHARD; BECK GERHARD
权利人:HOECHST AG
摘要:PCT No. PCT/EP93/02673 Sec. 371 Date May 15, 1995 Sec. 102(e) Date May 15, 1995 PCT Filed Sep. 30, 1993 PCT Pub. No. WO94/00789 PCT Pub. Date Apr. 14, 1994Process for the stereoselective synthesis of 3-substituted 2-thiomethylpropionic acids Compounds of the formula I I in which R1 and R2 are as defined can be prepared stereoselectively by reaction of acrylic acid or derivatives thereof or propionic acid or derivatives thereof with a chiral auxiliary, reaction with a mercaptan, stereoselective alkylation and subsequent hydrolysis and oxidation.

专利号:WO-2011106929-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人：MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO
权利人:MERCK SHARP & DOHME; ANGELETTI P IST RICHERCHE BIO; MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; HABERMANN JOERG; KOCH UWE; NARJES FRANK; LI PENG; PENG XUANJIA; SOLL RICHARD; WU HAO
摘要:Compounds of formula I that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infection and for inhibiting HCV viral replication and /or viral production in a cell-based system.

专利号:US-5498719-A
优先权日:1994-01-31
标题:Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors
发明人：MARQUEZ VICTOR E; DRISCOLL JOHN S; SIDDIQUI MAQBOOL A
权利人:US ARMY
摘要:The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-α-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.

专利号:US-2012328569-A1
优先权日:2010-03-02
标题:Inhibitors of hepatitis c virus ns5b polymerase
发明人：MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
权利人:MCCOMAS CASEY CAMERON; LIVERTON NIGEL J; SOLL RICHARD; LI PENG; PENG XUANJIA; WU HAO; NARJES FRANK; HABERMANN JOERG; KOCH UWE; LIU SHILAN
摘要:Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:WO-9407849-A1
优先权日:1992-10-01
标题:Process for the stereoselective synthesis of 3-substituted 2-thiomethyl propionic acids

专利号:DE-19813821-A1
优先权日:1998-03-20
标题 :Process for the production of C1-C6 building blocks for the total synthesis of epothilone and epothilone derivatives