📜3-(4-甲氧基苯氧基)-1,2-丙二醇置于水,氢溴酸,三苯基膦,偶氮二甲酸二乙酯体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 31.5H,反应生成 丙胺酚醇 参考文献:Effective Synthesis Of Non-Racemic Prenalterol Based On Spontaneous Resolution Of 3-(4-Hydroxyphenoxy)Propane-1,2-Diol 标题:Effective Synthesis Of Non-Racemic Prenalterol Based On Spontaneous Resolution Of 3-(4-Hydroxyphenoxy)Propane-1,2-Diol 摘要:Spontaneous Resolution Of Rac-3-(4-Hydroxyphenoxy)Propane-1,2-Diol Has Been Successfully Used In The Synthesis Of Both Enantiomers Of Chiral Drug Prenalterol. DOI:10.1016/j.Mencom.2019.03.028
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-4777293-A 优先权日:1984-08-13 标题 :Method for the synthesis of pharmacologically active compounds and intermediates for such synthesis 发明人:LAMM BO R 权利人:HAESSLE AB 摘要:A process for the preparation of an aryloxypropanolamine of the formula n n Ar--OCH.sub.2 CH(OH)CH.sub.2 NH--R I n n wherein Ar is a carbocyclic or heterocyclic aromatic group and R is an alkyl or substituted alkyl group having 1 to 6 carbon atoms, characterized in subjecting a compound of the formula ##STR1## to oxidative cleavage to a dialdehyde of the formula ##STR2## which is then made subject to reduction, amination, acetal hydrolysis, and, where required, removal of a nitrogen protective group, to the formation of a compound of formula I, or an acid addition salt thereof, a compound of formula II and the preparation thereof from mannitol.
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.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
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