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-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
专利号:US-6608202-B1 优先权日:2001-08-21 标题:Process of synthesis of a tricyclic ketone intermediate 发明人:DORAN HENRY J; O'NEILL PAT M; WILLIAMS ROBERT P 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of a compound of Formula III, wherein X is halogen,and intermediates therefor from easily available starting materials by a simple route.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-7919505-B2 优先权日:2006-07-11 标题 :Xinafoate salt of a substituted 5-oxazol-2-yl-quinoline compound 发明人:TING PAULINE C; LEE JOE F; FENG KUNG-I; REEDER MICHAEL R; TRZASKA SCOTT T; ZHU MAN; MAO CHEN; FILIPOV DIMITAR L; ZARKADAS DIMITRIOS N 权利人:SCHERING CORP 摘要:The present invention relates to the compound of the formula n nTo methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to polymorphs and processes of synthesis of the polymorphic forms.
专利号:US-2011003780-A1 优先权日:2007-07-10 标题:Hydrogen chloride salt of a substituted 5-oxazol-2-yl-quinoline compound and a process for the production thereof 发明人:ZHU MAN 权利人:SCHERING CORP 摘要:The present invention relates to the compound of the Formula I: n n n n n n n n n n and to methods of treating upper and lower obstructive airway diseases using said compound, to formulations comprising it, and to a particular crystalline form and processes of synthesis of the crystalline form. n IM=105109
1: Zhang K, Zhang XQ, Lu W, Xie HR, He L, Jiang XH, Wang L. [Determination of Desloratadine and Its Metabolite 3-OH Desloratadine in Human Plasma by LC-MS/MS]. Sichuan Da Xue Xue Bao Yi Xue Ban. 2015 Sep;46(5):783-7, 804. Chinese. doi: 10.1016/j.jval.2015.09.1376. Epub 2015 Oct 20. doi: 10.1016/j.ejphar.2015.10.014. Epub 2015 Oct 9. doi: 10.1007/s40261-015-0343-1. doi: 10.1124/dmd.115.065011. Epub 2015 Jul 1. doi: 10.1016/j.ejphar.2015.02.016. Epub 2015 Feb 19. doi: 10.1124/dmd.114.062620. Epub 2015 Jan 16.
合成参考文献
参考文献:10.3797/scipharm.1012-13 摘要:Ramulu G, Ravindra Kumar Y, Vyas K, Suryanarayana MV, Mukkanti K. A new validated liquid chromatographic method for the determination of loratadine and its impurities. Sci Pharm. 2011 Apr;79(2):277–91. 摘要:Authried G, Bracher L, Bygum A. [Urticaria multiforme is a variation of urticaria, which imitates erythema multiforme]. Ugeskr Laeger. 2013 Feb 11;175(7):436–7.