CAS: 18559-94-9; Albuterol

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CAS号24085-03-8 4-(2-(苄基(叔丁基)氨基... | CAS号90-02-8 水杨醛 | CAS号75-64-9 叔丁胺 | CAS号115787-51-4 Benzaldehyde, 5... | CAS号115787-50-3 5-(2-溴乙酰基)-2-羟基苯甲醛 | CAS号115787-57-0 2-Chloro-1-[3-[... | CAS号115787-56-9 2-Bromo-1-[3-[[... | CAS号115787-53-6 5-[[(1,1-Dimeth... | CAS号24085-03-8 4-(2-(苄基(叔丁基)氨基...

在 Palladium 10% On Activated Carbon,氢气体系中,用 四氢呋喃 用作溶剂,化学反应 12.0H,以86%的收率获得沙丁胺醇
参考文献:一种消旋沙丁胺醇的制备方法
标题:一种消旋沙丁胺醇的制备方法
摘要:本发明公开了一种消旋沙丁胺醇的制备方法,以5‑溴水杨醛为原料,与硼氢化钠经还原反应,得到中间体i;中间体i与氢化钠,卤化苄经烷基化反应,得到中间体ii;中间体ii与乙烯基三氟硼酸钾经交叉偶联反应,得到中间体iii;中间体iii与n‑溴代琥珀酰亚胺经加成反应,得到中间体iv;中间体iv与叔丁胺经烷基化反应,得到中间体v;中间体v在氢气氛围下发生脱保护反应,得到消旋沙丁胺醇.首次采用5‑溴水杨醛为反应原料降低生产成本,通过溴原子的引入,可使反应在5位上定向引入官能团,提高了反应的选择性和收率;不涉及高危剧毒试剂;首次将suzuki‑miyaura交叉偶联反应用于沙丁胺醇的合成中,使用催化量的钯催化剂,便可实现芳环上双键的高效引入,提高反应收率的同时降低了成本.

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-11053227-B2
优先权日:2017-12-20
标 题:Process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction and novel synthesis intermediates
发明人：COLLI CORRADO; BERTOLINI GIORGIO; SADA MARA; GARIS FARIS; NISIC FILIPPO; BIANCHI ALDO; BIAGGI CINZIA; DI FABIO ROMANO; RONZONI SILVANO; BERTUOLO STEFANIA; PRANDI ADOLFO; MAIORANA STEFANO
权利人:OLON SPA
摘要:Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2006167025-A1
优先权日:2004-12-22
标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs
发明人：BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.

专利号:US-11311505-B2
优先权日:2017-02-24
标 题:Synergistic compositions to stimulate the synthesis of human lung and sinus surfactants to decrease coughing, increase FEV-1/FVC ratios, decrease lung fibrosis, by increasing apoptosis of myofibroblasts
发明人：MARTIN ALAIN
权利人:MARTIN ALAIN; CELLULAR SCIENCES INC
摘要:Methods for the treatment of patients with both Chronic Obstructive Pulmonary Disease (COPD) and pulmonary fibrosis, and of patients with idiopathic pulmonary fibrosis without COPD, by stimulating the synthesis of human and animal patient lung and sinus surfactants to increase lung functions, inhibiting fibrosis and reducing coughing and nasal erythema, include the following steps: A) analyzing and diagnosing a patient with a lung ailment selected from the group consisting of i) both COPD and pulmonary fibrosis; and ii) idiopathic pulmonary fibrosis without COPD; and, B) treating the patient to raise the patient's lung functions including FEV1/FVC ratio by contacting mammalian cells with a [therapeutically effective amount of a treatment] composition that includes: a) a pyruvate salt; b) a phosphate; c) a salt of calcium; and d) a salt of magnesium, in an aqueous carrier, containing no more than 2.2 grams of said pyruvate salt per liter.

专利号:US-5442118-A
优先权日:1994-04-22
标题 :Asymmetric synthesis of (R)- and (S)-arylethanolamines from iminoketones
发明人：GAO YUN; HONG YAPING; ZEPP CHARLES M
权利人:SEPRACOR INC
摘要:A method for the enantioselective reduction of an alpha -iminoketone to an alpha -aminoalcohol is disclosed. The method utilizes a borane reducing agent as the reducing agent and a chiral 1,3,2-oxazaborole as the catalyst. The method is applied to the synthesis of R-albuterol from methyl 5-acetylsalicylate in high yield and high optical purity.