专利号:US-9409945-B2 优先权日:1999-10-04 标 题 :Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery 发明人:DESLONGCHAMPS PIERRE; DORY YVES; BERTHIAUME GILLES; OUELLET LUC; LAN RUOXI 权利人:OCERA THERAPEUTICS INC 摘要:A library of macrocyclic compounds of the formula (I) n n n n n n n n n n n n where part (A) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) y — bivalent radical or a covalent bond; n where part (B) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) z — bivalent radical, or a covalent bond; n where part (C) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) t — bivalent radical, or a covalent bond; and n where part (T) is a —Y-L-Z— radical wherein Y is CH 2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.
专利号:US-5919971-A 优先权日:1996-11-22 标题:Process for the synthesis of 3-mercaptopropionic acid esters 发明人:ARRETZ EMMANUEL 权利人:ELF AQUITAINE EXPLORATION PROD 摘要:This process for the synthesis of 3-mercaptopropionic acid esters by addition reaction of H2S to the corresponding acrylic acid ester is carried out in the presence of a solid-support functionalized with basic guanidine functional groups, on condition that these groups are free of hydrogen that is directly attached to a nitrogen atom.
专利号:US-11766432-B2 优先权日:2018-07-27 标题 :Cleavable conjugates of catechol compounds and water-soluble polymers and methods of treatment using the same 发明人:BENTLEY MICHAEL; FANG ZHIHAO; WEIMER REBECCA; VIEGAS TACEY; MOREADITH RANDALL 权利人:SERINA THERAPEUTICS INC 摘要:Described are conjugates comprising a water-soluble polymer linked to a compound comprising a catechol moiety via a cleavable linkage, wherein the cleavable linkage is formed between the water-soluble polymer and a first phenolic hydroxyl group of the catechol moiety and a second phenolic hydroxyl group of the catechol moiety is linked to a blocking group wherein the rate of hydrolytic release of the compound comprising the catechol moiety is controlled, at least in part, through structure or design of the blocking group on the second phenolic hydroxyl group of the catechol moiety. Therefore, the rate of hydrolytic release of the compound comprising the catechol moiety can be tuned through structural design of the group on the second phenolic hydroxyl group of the catechol moiety. Compounds used in the synthesis of the described conjugates and methods of using the described conjugate and other compounds in the treatment of dopamine-responsive disorders are also described.
专利号:US-5922910-A 优先权日:1997-08-27 标 题 :Synthesis of carboxyalkylthiosuccinic acids 发明人:LABAT YVES; MULLER JEAN-PIERRE 权利人:ATOCHEM ELF SA 摘要:Process for the preparation of a carboxyalkylthiosuccinic acid of formula ##STR1## in which n=1 to 3 and Râ• H or CH 3 , a mercapto ester of formula HS--(CH 2 ) n --COOR' in which R' is a C 1 to C 4 alkyl radical, is reacted, in aqueous medium and without a catalyst, with maleic acid, citraconic acid or their anhydride. The invention is more particularly directed towards the preparation of carboxyethylthiosuccinic acid (CETSA).
专利号:US-5698600-A 优先权日:1995-10-24 标题:Process for the production of bisphenols with the use of new cocatalysts 发明人:WULFF CLAUS; FENNHOFF GERHARD; EITEL ALFRED 权利人:BAYER AG 摘要:The invention relates to the synthesis of bisphenols from monophenols and carbonyl compounds such as aldehydes and ketones with concentrated mineral acids such as hydrochloric acid and/or hydrogen chloride gas as acid catalysts and a mercaptan as cocatalyst, which is fixed by an ion-pair bond to a matrix insoluble in the reaction medium.
专利号:US-12441760-B2 优先权日:2013-08-29 标 题 :Amino diacids containing peptide modifiers 发明人:BARLOS KLEOMENIS; GATOS DIMITRIOS; BARLOS KOSTAS K; VASILEIOU ZOI 权利人:CHEMICAL & BIOPHARMACEUTICAL LABORATORIES OF PATRAS S A 摘要:The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.
[参考文献]: Ashish Punia, Et Al. Effect Of Relative Arrangement Of Cationic And Lipophilic Moieties On Hemolytic And Antibacterial Activities Of Pegylated Polyacrylates. Int J Mol Sci. 2015 Oct 9;16(10):23867-80. [参考文献]: Thomas M Kohl, Et Al. Amination Of Aryl Halides And Esters Using Intensified Continuous Flow Processing. Molecules. 2015 Sep 25;20(10):17860-71.
合成参考文献
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