1,2;5,6-Di-O-Isopropylidenmannit置于sodium Periodate,碳酸氢钠体系中,用 二氯甲烷 用作溶剂,化学反应 6.0H,以42%的收率获得(R)-(+)-2,2-二甲基-1,3-二氧戊环-4-甲醛 参考文献: Process For The Preparation Of A Fluorolacton Derivative[fr] Procédé De Préparation D'Un Dérivé De Fluorolactone 标题: Process For The Preparation Of A Fluorolacton Derivative[fr] Procédé De Préparation D'Un Dérivé De Fluorolactone 摘要:描述了一种制备公式(i)的氟内酯衍生物和其酰化衍生物的新工艺,其中r1代表一个羟基保护基团.公式(v)的酰化氟内酯,特别是r1 =苄基的苯甲酰衍生物,是合成前药化合物的重要前体,这些前药化合物具有潜力成为对丙型肝炎病毒(hcv)ns5B聚合酶具有强效抑制作用的化合物.
专利号:WO-2006095359-A1 优先权日:2005-03-10 标题:Synthesis of 2-deoxy-2, 2-di fluoro-d-ribo furanose-3, 5 di(4-methy/4-nitro-chloro)benzoate and its conversion to gemcitabine hydrochloride thereof 发明人:POTLURI RAMESH BABU; VENKATA SUBRAMANIAN HARIHARAKR; BETINI RAMESH; GUNTURU SATYANARAYANA 权利人:SMS PHARMACEUTICALS LTD; POTLURI RAMESH BABU; VENKATA SUBRAMANIAN HARIHARAKR; BETINI RAMESH; GUNTURU SATYANARAYANA 摘要:The invention describes the synthesis of hereto unreported 2-deoxy-2,2-difluoro-D-ribofuranose-3,5-di-(aroyl) derivative of formula-Vb, where in R=;CH3,CI,NO2 and its conversion to Gemcitabine HCl of formula-I, an anti cancer product.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
专利号:US-2015031898-A1 优先权日:2012-03-09 标题 :Process for preparation of prostaglandin f2 alpha analogues 发明人:DAMS IWONA; KUTNER ANDRZEJ; CHODYNSKI MICHAL; KRUPA MALGORZATA; PIETRASZEK ANITA; ZEZULA MARTA; CMOCH PIOTR; KOSINSKA MONIKA 权利人:INST FARMACEUTYCZNY 摘要:A convergent synthesis of the prostaglandin F 2α analogues, travoprost and bimatoprost, was developed employing Julia-Lythgoe olefination of the structurally advanced phenylsulfone with an enantiomerically pure aldehyde ω-chain synthon. The novel convergent strategy allows the synthesis of a whole series of prostaglandin analogues of high purity from a common and structurally advanced prostaglandin intermediate.
专利号:US-7084281-B2 优先权日:2003-01-22 标题:Synthesis of dihalohydrins and tri- and tetra-substituted olefins 发明人:FALCK JOHN R; BARMA DEB K; KUNDU ABHIJIT 权利人:UNIV TEXAS 摘要:A novel synthesis reaction for highly stereospecific tri- and tetra-substituted olefins is described. A single stereoisomer of stable α-halo-α,β-ester is produced in high yield by the reaction of aldehyde or ketone with a trihalogenated compound such as trichloroacetate in the presence of CrCl 2 in a solvent. By varying the amount of CrCl 2 used, the stable dihalohydrin intermediate may be obtained as well.
专利号:US-2007042987-A1 优先权日:2004-07-30 标题:Stereoselective synthesis of beta-nucleosides 发明人:LIN KO-CHUNG; LI WENSEN; LIN CHUNHUI; YUNGSHUN WEIN; KUO-HIS KAO 权利人:LIN KO-CHUNG; LI WENSEN; LIN CHUNHUI; YUNGSHUN WEIN; KUO-HIS KAO 摘要:This invention relates to a process of stereoselectively synthesizing an alcohol of the following formula: n n nwherein R 1 , R 2 , R 3 , R 4 , and R 5 are defined in the specification. The process includes reacting (R) 4-formyl-2,2-dimethyldioxolane with α-bromoacetate in the presence of Zn and a Zn activating agent.
专利号:US-7485716-B2 优先权日:2005-05-02 标题:Stereoselective synthesis of β-nucleosides 发明人:LIN KO-CHUNG; LI WENSEN 权利人:PHARMAESSENTIA CORP 摘要:This invention relates to a process for stereoselectively preparing a nucleoside of the following formula: n nwherein R 3 , R 4 , and B are defined herein. The process includes reacting a furanose compound with a nucleobase in the presence of a halide salt. Also disclosed is another process for stereoselectively synthesizing an intermediate that can be used to make the starting compound in the first-mentioned process.
参考标题:Total Synthesis Of (−)-21-Isopentenylpaxilline 作者:Amos B. Smith,Haifeng Cui |发布日期:2003.2.1 摘要:[structure: See Text] The Total Synthesis Of (-)-21-Isopentenylpaxilline (1) Has Been Achieved. Key Elements Of The Synthesis Include The Stereocontrolled Construction Of The Advanced Eastern Hemisphere (-)-5, A Highly Efficient Union Of The Eastern And Western Fragments (-)-5 And 4, Respectively, Exploiting Our 2-Substituted Indole Synthesis, And A New Protocol For The Construction Of Ring C.
合成参考文献
摘要:Yliniemelä-Sipari, S. M.; Piisola, A.; Pihko, P. M., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 64. 参考文献:10.1021/jo0257905 摘要:Rassu G, Auzzas L, Pinna L, Zambrano V, Zanardi F, Battistini L, Marzocchi L, Acquotti D, Casiraghi G. Variable strategy toward carbasugars and relatives. 4. Viable access to (4a-carbapentofuranosyl)amines, (5a-carbahexopyranosyl)amines, and amino acids thereof. J Org Chem. 2002 Jul 26;67(15):5338–42. doi: 10.1021/jo0257905. 参考文献:10.1021/jo0499118 摘要:Wicha J, Zarecki A. Olefination of alpha-hydroxy or alpha-aminoaldehyde derivatives via reaction of their arylsulfonylhydrazones with sulfonyl anions. J Org Chem. 2004 Aug 20;69(17):5810–2. doi: 10.1021/jo0499118.