专利号:US-7619116-B2 优先权日:2003-12-17 标 题:Intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation 发明人:DAMBRIN VALERY; LENOIR JEAN-YVES; SCHNEIDER JEAN-MARIE; GUILLAMOT GERARD; FOLLET MICHEL; BECKER ABRAM 权利人:PRODUCTS CHIMIQUES AUXILIAIRES 摘要:A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.
专利号:US-5801047-A 优先权日:1992-11-25 标题:Method for making stable extracellular tyrosinase and synthesis of polyphenolic polymers therefrom 发明人:DELLA-CIOPPA GUY RICHARD; GARGER JR STEPHEN JOHN; HOLTZ RICHARD BARRY; MCCULLOCH MICHAEL JAY; SVERLOW GENADIE GLEB 权利人:BIOSOURCE TECH INC 摘要:A process for the in vitro production of chemically modified polyphenolic polymer (PPP). First, stable, highly active extracellular tyrosinase is produced from genetically transformed microorganism such as Streptomyces antibioticus. The tyrosinase is then incubated with a reaction substrate such as 1-tyrosine, hydrolyzed protein, or an oligopeptide in combination with 1-tyrosine. The ratio of the oligopeptide/tyrosine combination as well as variation in the concentration of tyrosinase can be used to modify the color, the molecular size, and the spectral absorbance properties of the PPP produced. Alternatively, or additionally, oxidants such as hydrogen peroxide or hypochlorite can be used to modify the color of the PPP, regardless of the method used to produce the PPP, and the PPP can subsequently be fractionated using molecular weight cut-off ultrafiltration. Organic solvents can also be used in the method of making PPP to produce PPPs having variable but reproducible physical properties.
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-2009234012-A1 优先权日:2002-03-21 标题 :Administration of dopa precursors with sources of dopa to effectuate optimal catecholamine neurotransmitter outcomes 发明人:HINZ MARTIN C 权利人:HINZ MARTIN C 摘要:A method of treating neurotransmitter dysfunction in a patient by optimizing catecholamine levels by administration of L-3,4-dihydroxyphenylalanine (L-Dopa or Dopa) precursors in combination with a source of L-Dopa. The dopa precursor is preferably administered in such quantities such that the amount of dopa from the dopa precursors does not fluctuate and affect outcomes in the synthesis of dopamine from dopa administration. The dopa precursor source is preferably tyrosine, but may alternatively be phenylalanine, N-acetyl-tyrosine, any active isomer thereof, or any other dopa precursor. The source of L-Dopa may include any natural or synthetic source, including, but not limited to, Mucuna pruriens.
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-5200546-A 优先权日:1991-09-30 标 题 :Phosphonoalkyl phenylalanine compounds suitably protected for use in peptide synthesis 发明人:BURKE JR TERRENCE R; LIM BENJAMIN B 权利人:US HEALTH 摘要:There are disclosed novel compounds of the formula: ##STR1## wherein, x is --CH 2 --, --CHF--, --CF 2 , --CHOH-- or --C(O)--; n R 6 is hydrogen, benzyl, pentafluorophenyl, nitrophenyl, 1-benzotriazolyl or 1-succinimidoyl; n Fmoc is 9-fluorenylmethyloxycarbonyl; and n * indicates a chiral carbon atom. n The Formula (I) compounds are useful in synthesizing peptides. There are also disclosed novel synthesis methods which include the step of hydrogenating a compound of the Formula ##STR2## wherein R 4 and R 5 are C 1-8 lower alkyl, to give a compound of the formula ##STR3## wherein R 4 and R 5 are as defined above. The compounds of formula (II) are useful as intermediates in preparing certain formula (I) compounds.
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合成参考文献
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