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-4389489-A 优先权日:1979-07-07 标 题:Optically pure heterocyclic aminoacid compounds, a process for their use for the synthesis of medicaments 发明人:PREISS MICHAEL; SCHUTT HERMANN 权利人:BAYER AG 摘要:The invention relates to optically pure heterocyclic amino acid compounds of the Formula I, as described hereinabove as well as a process for their preparation involving subject D, L-compounds to the action of a proteolytic enzyme. The compounds obtained are useful, inter alia, as intermediates for the manufacture of cephalosporins or penicillins.
专利号:EP-1734036-B1 优先权日:2005-06-14 标 题:Process for preparation of tamsulosin and its derivatives 发明人:JIH RU HWU; MAGENDRAN BALAACHARY; CHAKRABORTY SUBHASISH K; DAS ASISH R; TSAY SHWU CHEN; SHEU KUEN WANG; SHU CHUN MEI; LU CHIN KUN; CHANG WEI MIN 权利人:WELL BEING BIOCHEMICAL CORP; TAIWAN BIOTECH CO LTD 摘要:The present invention discloses a new process for the synthesis of tamsulosin derivatives of formula 1 (where R 1 and R 2 represent C 1 -C 4 alkyl groups) and their hydrochlorides and other pharmaceutically acceptable salts, comprising reacting the hydrochloride of sulphonamide 2 (where R represents C 1 -C 4 alkyl) with the ether compound 21 (where R' represents C 1 -C 4 alkyl and R' represents MeC 6 H 4 SO 2 or MeSO 2 ).
专利号:US-5304631-A 优先权日:1990-01-16 标题:Synthetic helizyme enzymes 发明人:STEWART JOHN M; HAHN KARL W; KLIS WIESLAW A 权利人:UNIV COLORADO FOUNDATION 摘要:The design, and synthesis of peptide-based molecules termed helizymes which possess catalytic activity are described herein The catalytic molecules of the invention comprise a number of amphiphilic helical peptides, which interact via hydrophobic interactions and which are bonded at their carboxyl ends to a multifunctional base. Active site residues functional for catalysis are positioned within or at the N-termini of the helical peptides. The helizyme molecule adopts a conformation in aqueous medium such that a substrate binding pocket is formed and such that functional active site geometry results from the association of the helical peptides Specifically exemplified helizymes possess specificities and at least one catalytic activity of chymotrypsin, trypsin and acetylcholine esterase.
专利号:CA-1148884-A 优先权日:1979-07-07 标 题:Optically pure heterocyclic aminoacid compounds, a process for their production and their use for the synthesis of medicaments
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合成参考文献
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