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肉豆蔻酸置于氯化亚砜体系中,化学反应 1.0H,以90%的收率获得肉豆蔻酰氯
参考文献:高聚合度的肉豆蔻酰基-氨基甲酸酯(dethia)-辅酶a的合成.
标题:高聚合度的肉豆蔻酰基-氨基甲酸酯(dethia)-辅酶a的合成.
摘要:各种信号蛋白的n端甘氨酸残基的共翻译肉豆蔻酰基化是膜附着和这些分子正常功能所必需的.N-肉豆蔻酰基转移酶(nmt)催化肉豆蔻酸从肉豆蔻酰基辅酶a(myr-Coa)的转移.Nmt与多种人类疾病有关,包括癌症和癫痫病以及诸如真菌和病毒感染(包括hiv和b型肝炎)的致病机制.合理的设计已导致开发了有效的竞争性抑制剂,包括几种非甾体抗炎药.可水解的酰基辅酶a底物类似物.然而,遵循原始coa合成路线的线性合成策略,在通常不适合于体内研究的所有产量上,以非常低的收率生成此类类似物.在这里,我们提出一个新的,肉豆蔻酰基-氨基甲酸酯(dethia)-辅酶a 1的高度收敛合成,与报道的线性合成相比,该合成物可以以11倍增加的收率获得这种底物类似物.另外,在合成的最后一步中,对2',3'-环磷酸腺苷的酶切被证明是获得异构纯3'-磷酸1的有效方法.
Doi:10.1002/ejoc.200901410

专利信息

专利号:US-7189849-B2
优先权日:1997-02-10
标 题:Synthesis of acyclic nucleoside derivatives
发明人：LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY
权利人:MEDIVIR AB
摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

专利号:US-3959322-A
优先权日:1960-09-22
标 题:Synthesis of 13-alkyl-gon-4-ones
发明人：HUGHES GORDON ALAN; SMITH HERCHEL
权利人:SMITH HERCHEL
摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.

专利号:US-2014371316-A1
优先权日:2011-11-23
标 题:Derivatives of phenoxyisobutyric acid
发明人：LALEZARI IRAJ; FABRICANT JILL S
权利人:FABRICANT JILL S; LALEZARI IRAJ
摘要:The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

专利号:US-2005095280-A1
优先权日:2003-10-15
标 题:Single-component pH-sensitive liposomes of reduced solid-to-liquid phase transition temperatures
发明人：SAVVA MICHALAKIS
权利人:MICHALAKIS SAVVA
摘要:The current invention relates to the synthesis of novel cationic lipids and their use as delivery vectors for nucleic acids, peptides and other synthetic drugs, in vitro and in vivo. The cationic lipids described herein form stable lamellar structures (liposomes) at physiological pH but destabilize to micelles at acidic and alkaline pH. These structures are characterized of high elasticity, increased fluidity and high transfection activity relative to the corresponding 1,2-dialkyl cationic derivatives and other phospholipids analogues.

专利号:US-2019031650-A1
优先权日:2016-01-29
标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies
发明人：HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN
权利人:UNIV YALE
摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.

专利号:US-2025122424-A1
优先权日:2023-10-13
标 题 :Low phonon energy nanoparticles based on alkali lead halides and methods of synthesis and use
发明人：ZHANG ZHUOLEI; SKRIPKA ARTIOM; SCHUCK P JAMES; COHEN BRUCE; CHAN EMORY
权利人:UNIV CALIFORNIA; UNIV COLUMBIA; UNIV MADRID AUTONOMA
摘要:Phonon engineered, lanthanide doped upconverting nanoparticles with very low phonon energies and tunable methods of synthesis that adjust OA:OM ratio and reaction temperature are provided. Low phonon energy KPb2X5 (X=Cl, Br) upconverting nanoparticles, both doped and undoped, exhibit dramatically suppressed multiphonon relaxation, enhancing upconversion emission from higher lanthanide excited states and enabling room temperature observation of avalanche like upconversion by Nd3+ ions. Intrinsic optical bistability (IOB) of the materials can provide bit level functionality to all optical computing. The IOB of Nd3+ doped nanocrystals, which are either bright or dark at the same excitation power based on power history, illustrate the functionality. High contrast switching and IOB are enabled via the photon avalanche process, which sustains population inversion between the ground and the first excited 4fN states of Nd3+ ions. The IOB of these nanocrystals can be controlled by temporal pump modulation and can store information.