CAS: 187227-45-8; (3R,4R,5S)-4-Acetamido-5-Amino-3-(Pentan-3-Yloxy)Cyclohex-1-Enecarboxylic Acid

上下游产品

methyl (3R,4R,5S)-4-acetamido-5-amino-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate oseltamivir 2-pentanol ethyl-(3R,4R,5S)-4-amino-5-azido-3-(pentan-3-yloxy)cyclohex-1-ene-1-carboxylate(3R,4R,5S)-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid trifluoroacetate (3R,4R,5S)-4-acetamido-5-[(tert-butoxycarbonyl)-amino]-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid

磷酸奥司他韦置于碳酸氢钠,水,Potassium Hydroxide体系中,用 甲醇 用作溶剂,化学反应生成奥司他韦酒石酸盐
参考文献:达菲的正式合成:达菲转化为磷酰胺
标题:达菲的正式合成:达菲转化为磷酰胺
摘要:柴的第三代中间的短,对映体,合成而形成(-)-奥司他韦磷酸盐(达菲®)已在八个步骤与使用便宜的起始原料已经实现.已经完成了通过方氏的tamiphosphor中间体将tamiflu转化为tamiphosphor的正式合成途径. 水解-环氧-氧化-酰胺-对映选择性
Doi:10.1055/s-0031-1290356

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-7888337-B2
优先权日:2007-08-31
标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity
发明人：WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG
权利人:ACADEMIA SINICA
摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.

专利号:US-11628186-B2
优先权日:2017-02-24
标题 :Method and composition for the reduction of viral replication, duration and spread of the COVID-19 and the flu
发明人：MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:A method for stimulating the synthesis of nasal nitric oxide and nasal and lung surfactants to inhibit the docking and adhesion of viruses to cellular receptors, including ACE2, to reduce viral replication, duration, spread and severity of infections, and also to inhibit lung fibrosis, increase the synthesis of serotonin to reduce coughing and mouth breathing, reduce the cytokine storm produced by LI-6 caused by viruses such as COVID-19 and flu in patients susceptible to these infections, including patients with hypoxemia, asthma, chronic obstructive pulmonary disease, cystic fibrosis, diabetics, interstitial lung disease, pulmonary fibrosis, allergic rhinitis, sinusitis, smokers, sleep apnea and lung cancer, which includes: contacting mammalian cells with a therapeutically effective amount of a composition, said composition including the following constituents: sodium pyruvate; a phosphate; a salt of calcium; and a salt of magnesium.

专利号:US-7977077-B2
优先权日:2006-01-30
标题:Synthesis of intermediates of oseltamivir carboxylates
发明人：FROST JOHN W; GUO JIANTAO
权利人:UNIV MICHIGAN STATE
摘要:Enzymatic pathways for production of aminoshikimate, kanosamine, intermediates, and derivatives thereof; nucleic acid encoding and cells containing the enzymes; compositions containing aminoshikimate, kanosamine, an intermediate or derivative thereof; and use of the cells and pathways for biosynthetic production of aminoshikimate, kanosamine, intermediates, and derivatives thereof.

专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:US-10385010-B1
优先权日:2018-03-28
标 题 :Expedient synthesis of oseltamivir and related compounds via direct olefin diazidation-diamidation reaction
发明人：XU HAO; LI HONGZE; SHEN SHOUJIE; ZHU CHENGLIANG
权利人:UNIV GEORGIA STATE RES FOUND
摘要:Disclosed herein are improved methods for the preparation of oseltamivir, and intermediates useful thereto.