CAS: 111-64-8; Octanoyl Chloride

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CAS号124-07-2 辛酸 | CAS号79-37-8 草酰氯 | CAS号69151-13-9 3,3-dichloro-1,... | CAS号6304-39-8 辛酰肼 | CAS号50966-31-9 1,1-dichloro-1-... | CAS号111013-41-3 iodomethyl °Ctanoate | CAS号108377-41-9 1-(2-sulfanylid... | CAS号4747-81-3 异氰酸庚酯 | CAS号47162-00-5 4-正辛酰联苯 | CAS号335-35-3 2,2,3,3,4,4,5,5... | CAS号335-57-9 全氟正庚烷 | CAS号335-66-0 全氟辛酰氟 | CAS号335-36-4 全氟(2-丁基四氢呋喃) | CAS号30711-41-2 2-辛酰基噻吩 | CAS号220727-26-4 3-辛酰基硫代丙基三乙氧基硅烷

辛酸置于氯化亚砜体系中,化学反应生成辛酰氯
参考文献:可能用于抗类风湿关节炎的bergenin前药的合成,Ph依赖性,血浆和酶稳定性
标题:可能用于抗类风湿关节炎的bergenin前药的合成,Ph依赖性,血浆和酶稳定性
摘要:卑尔根是一个独特的c-糖苷天然产物具有抗炎和抗关节炎活性.它是亲水分子,在酸性条件下稳定,但是在中性碱性ph条件下不稳定.降解速率与ph值增加成正比,这可能是其口服生物利用度低的原因之一.因此,本文的目的是使用前药策略改善其稳定性.合成了各种酯和醚前药,并研究了它们在血浆/酯酶中的亲脂性,化学稳定性和酶促水解作用.在不同ph的缓冲液,生物相关培养基(如sgf,Sif,大鼠血浆和酯酶)中评估了合成前药的稳定性.所有的前药都显示出比bergenin显着改善的亲脂性,这符合类药物化合物的标准.乙酰酯4A 2似乎是最有前途的前药,因为它在胃/肠ph值下保持稳定,并根据理想前药的需要在血浆中完全转化为母体化合物bergenin.本文提供的数据将有助于设计结构相似的化学型中具有所需理化性质的不稳定分子的稳定前药.
Doi:10.1016/j.Bmc.2017.08.011

专利信息

专利号:US-9988364-B1
优先权日:2017-03-21
标题 :Process for synthesis of Eliglustat and intermediate compounds thereof
发明人：LIU YU; YU GUANNENG; ZHENG ZHIGUO
权利人:ZHEJIANG AUSUN PHARMACEUTICAL CO LTD
摘要:The present invention relates to a process for synthesis of Eliglustat and intermediate compounds thereof. In particular, the present invention relates to a process for synthesis of Eliglustat and pharmaceutically acceptable salts thereof, and relates to the intermediate compounds in the process and a process for preparation of the intermediate compounds.

专利号:WO-2013008044-A1
优先权日:2011-07-08
标题:Synthesis of (+) and (-) 1 -(5,5-diphenyltetrahydrofuran-3- yl)-n,n-dimethylmethanamine, (+) and (-) 1-(2,2-diphenyltetrahydrofuran-3-yl)-n,n- dimethylmethanamine and (+) and (-) 1-(2,2- dffhenyltetrahydrofuran-3-yl)-n-metihylmethanamine
发明人：WAMVAKIDES ALEXANDRE; MOUTSOS VASSILIOS; SCHMITT MARTINE
权利人:ANAVEX LIFE SCIENCES CORP; WAMVAKIDES ALEXANDRE; MOUTSOS VASSILIOS; SCHMITT MARTINE
摘要:The current invention covers the synthesis of (+) and (-) l-(5,5-diphenyItetrahydrofuran-3- yl)-N,N-dimethylmethanamine [(±)1] and [(-)1] respectively, including their pharmacologically acceptable acid addition salts. The new products can be synthesized starting from 5,5-diphenyltetrahydrofuran-2(3H)-one (4) after insertion of an aldehyde group in the α-position, reduction to the prochiral 3-(hydroxymethyl)-1, 1-diphenylbutane-1,4-diol (6), chemoenzymatic desymmetrization using the enzyme Amano Lipase PS30, tosylation, intramolecular nucleophilic attack, hydrolysis, reaction with trifluoromethanesulfonic anhydride and substitution by dimethylamine, thus producing (+) 1-(5,5-diphenyl- tetrahydrofuran-3-yl)-N,N-dimethylmethanamine [(+)1]. Protection of the product of the chemoenzymatic desymmetrization with tert-butyldimethylsilyl chloride, hydrolysis, tosylation, intramolecular nucleophilic attack, removal of tert-butyldimethylsilyl group, reaction with trifluoromethanesulfonic anhydride and substitution by dimethylamine produces (-) 1-(5,5-diphenyltetrahydrofuran-3-yl)-N,N-dimethylmethanamine [(-)1]. It also covers the synthesis of (+) and (-) 1-(2,2-diphenyltetrahydrofuran-3-yl)-N,N- dimethylmethanamine [(+)2] and [(-)2] respectively and (+) and (-) 1-(2,2-diphenyl- tetrahydrofuran-3-yl)-N-methylmethanamine \\(+)3] and [(-)3] respectively, including their pharmacologically acceptable acid addition salts. The new products can be synthesized either starting from the reduction of 5-oxo-2,2-diphenyltetrahydrofuran-3-carboxylic acid (13) with LiA1H 4 , followed by the cyclization of the obtained triol (14) under acidic conditions, reaction with 1S-(-) or1R-(+)camphanic chloride, recrystallization, hydrolysis, reaction with trifluoromethanesulfonic anhydride and substitution by dimethylamine or methylamine, or by the reaction of R-(-) or S-(+) Mandelic acid and acetic acid with racemic 1-(2,2-diphenyltetrahydrofuran-3-yl)-N,N-dimethylmethanamine (2), recrystallization, followed by reaction with an aqueous solution of NaOH. The compounds mentioned in the invention present neuroprotective, antiepileptic and antidepressant activity and can be used as therapeutic agents.

专利号:US-9546161-B2
优先权日:2001-07-16
标题:Synthesis of UDP-glucose: N-acylsphingosine glucosyl transferase inhibitors
发明人：HIRTH BRADFORD H; SIEGEL CRAIG
权利人:GENZYME CORP
摘要:Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

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:WO-2005040408-A1
优先权日:2003-10-22
标 题 :Method for the identification of enzymes having desired properties by immobilisation of the reaction product on the surface of enzyme-presenting organisms
发明人：KOLMAR HARALD
权利人:SELECORE GMBH; KOLMAR HARALD
摘要:The invention relates to a method for the identification of enzymes with a desired activity, by random generation of a large collection of enzyme variants, the synthesis of said variants in host organisms, the presentation thereof on the surface of the organisms and the isolation of enzyme variants with the desired properties, by the detection of the covalent deposition of the reaction product on the surface of the host organism.

专利号:US-12227522-B2
优先权日:2020-12-21
标题:Synthesis of structural analogs of largazole and associated compounds
发明人：WILLIAMS ROBERT M; KOTI SIVANAGIREDDY; DE SUBHADIP; SHELKE ANIL M; CERBONE RYAN E; YASUDA NOBUYOSHI
权利人:UNIV COLORADO STATE RES FOUND; CETYA THERAPEUTICS INC
摘要:Disclosed are various synthetic methods to prepare structural analogs of largazole and derivatives thereof. One structural analog is an amide isostere of largazole. Another structural analog replaces the thiazole ring of largazole with a pyridine moiety or an oxazole moiety. Also disclosed are various intermediate compounds obtained when preparing structural analogs of largazole and derivatives thereof, including macrocycle analogs having an alcohol functionality.