专利号:US-7282606-B2 优先权日:2005-07-13 标题:Process for preparation of tamsulosin and its aralkylamine derivatives 发明人:JIH RU HWU; TSAY SHWU CHEN; MAGENDRAN BALAACHARY; CHAKRABORTY SUBHASISH K; DAS ASISH R; SHEU KUEN WANG; SHU CHUN MEI; LU CHIN KUN; CHANG WEI MIN 权利人:TAIWAN BIOTECH CO LTD 摘要:The present invention discloses a new process for the synthesis of tamsulosin and its aralkylamine derivatives, especially (R)-(−)-5-{2-[2-(2-alkoxyphenoxy) ethylamino]propyl}-2-alkoxybenzenesulfonamides having the following formula 1 (where R 1 and R 2 represent C 1 -C 4 alkyl groups) and their hydrochloride thereof, and other various pharmaceutical used salts. n n n n n n n n n n Tamsulosin hydrochloride (R 1 =Et, R 2 =Me, in its hydrochloride salt form) is an antagonist of α-A adrenoceptors in the prostate. Tamsulosin•HCl occurs as white crystals, which melt with decomposition at approximately 230° C. It is sparingly soluble in water and in methanol, slightly soluble in glacial acetic acid and in ethanol, and practically insoluble in ether.
专利号:US-9783800-B2 优先权日:2014-02-03 标 题:Method for producing peptides having azole-derived skeleton 发明人:SUGA HIROAKI; GOTO YUKI; KATO YASUHARU 权利人:UNIV TOKYO 摘要:Object of the present invention is to develop an artificial synthesis system of various peptides having an azole derivative structure and develop a library of such peptides. The present invention provides a method of producing a peptide having, in the backbone thereof, an azole derivative structure comprising the step of: synthesizing a substrate peptide of an azoline structure introducing enzyme having, in the modified region thereof, at least any one of the following amino acids, n n[in any of the compounds,n X 1 represents a group selected from the group consisting of SH, OH, NH 2 , SR 1 , OR 1 , NHR 1 , and N 3 (R 1 represents a protecting group), X 2 represents an easily eliminable group; and X 3 represents hydrogen or a substituted or unsubstituted alkyl or aryl group having from 1 to 10 carbon atoms]; reacting the substrate peptide with an azoline structure introducing enzyme to obtain a peptide having an azoline derivative structure; and converting the azoline derivative structure of the resulting peptide into an azole derivative structure by inducing an HX 2 elimination reaction of X 2 group.
参考标题:Process For Preparation Of Tamsulosin And Its Aralkylamine Derivatives 摘要:The Present Invention Discloses A New Process For The Synthesis Of Tamsulosin And Its Aralkylamine Derivatives, Especially (R)-(−)-5-2-[2-(2-Alkoxyphenoxy)Ethylamino]Propyl}-2-Alkoxybenzenesulfonamides Having The Following Formula 1 (Where R 1 And R 2 Represent C 1 -C 4 Alkyl Groups) And Their Hydrochloride Thereof, And Other Various Pharmaceutical Used Salts. Tamsulosin Hydrochloride (R 1 =et, R 2 =me, In Its Hydrochloride Salt Form) Is An Antagonist Of α-A Adrenoceptors In The Prostate. Tamsulosin.hcl Occurs As White Crystals, Which Melt With Decomposition At Approximately 230° C. It Is Sparingly Soluble In Water And In Methanol, Slightly Soluble In Glacial Acetic Acid And In Ethanol, And Practically Insoluble In Ether.
合成参考文献
参考文献:10.1021/jm00027a027 摘要:Ye QZ, Johnson LL, Nordan I, Hupe D, Hupe L. A recombinant human stromelysin catalytic domain identifying tryptophan derivatives as human stromelysin inhibitors. J Med Chem. 1994 Jan 07;37(1):206–9. doi: 10.1021/jm00027a027.