CAS: 54-49-9; Metaraminol

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meta-hydroxybenzaldehyde (R)-1-hydroxy-1-(3-hydroxyphenyl)propan-2-one (+/-)-1-hydroxy-1-(3-hydroxy-phenyl)-acetone oxime RS:2SR)-2-amino-1-(3-benzyloxy-phenyl)-propanol-(1)(1RS:2SR)-2-amino-1-(3-benzyloxy-phenyl)-propanol-(1)(1R,2S)-2-amino-1-(3-hydroxy-4-iodophenyl)-1-propanol (1R,2S)-2-(tert-butoxycarbonylamino)-1-(3-hydroxyphenyl)-1-propanol

📜(1R,2S)-N-(Benzyloxycarbonyl)-2-Amino-1-(3-Benzooxyphenyl)-1-Propanol置于palladium On Activated Charcoal,氢气体系中,用 甲醇,二氯甲烷 作为反应溶剂,以98%的收率获得产物间羟胺
参考文献:重酒石酸间羟胺的合成方法
标题:重酒石酸间羟胺的合成方法
摘要:本发明提供了一种重酒石酸间羟胺的合成工艺,以苄氧羰基‑l‑丙氨酸为原料,进行环合反应,并与格式试剂反应,制得中间体,(4S)‑n‑苄氧羰基‑5‑(3‑(卞氧基)苯基)‑5‑羟基‑4‑甲基恶唑烷;中间体进行水解开环反应,反应生成(2S)‑2‑(苄氧羰基)氨基‑1‑(3‑苄氧基苯基)‑1‑丙酮;将(2S)‑2‑(苄氧羰基)氨基‑1‑(3‑苄氧基苯基)‑1‑丙酮进行还原反应,高选择性得到(1R,2S)‑2‑(苄氧羰基)氨基‑1‑(3‑卞氧基苯基)‑1‑丙醇;对其进行脱保护,得到间羟胺;最后通过间羟胺与l‑酒石酸成盐,得到重酒石酸间羟胺.本方法避免了使用昂贵的催化剂和手性拆分,大大的降低了成本;使利用化学合成,工业生产光学纯重酒石酸间羟胺成为可能.

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-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-5962737-A
优先权日:1997-01-08
标 题 :2-amino-1-phenylpropanols, stereospecific synthesis thereof, and method of optically resolving the same
发明人：WEST DANIEL DAVID
摘要:Stereospecific synthesis of the racemic threo isomers of 2-nitro-1-phenylpropanols by reacting a benzaldehyde derivative with nitroalkane in the presence of a tertiary amine and reducing 2-nitro-1-phenylpropanols with, for example, lithium aluminum hydride to 2-amino-1-phenylpropanols is described. Also described are phase transfer resolution of racemic mixtures of 2-amino-1-phenylpropanol and its derivatives into their optically pure isomers by reacting a racemic mixture with the mono alkali metal salt of a tartaric acid ester in a two phase system of a hydrocarbon and water. The specification further describes therapeutically useful optically pure isomers of threo-2-amino-1-(dialkoxy or alkoxy) phenylpropanols and acid addition salts thereof.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-8017776-B2
优先权日:2003-07-15
标题 :Methods for synthesis of acyloxyalkyl compounds
发明人：BHAT LAXMINARAYAN; GALLOP MARK A
权利人:XENOPORT INC
摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

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.