专利号:US-12435042-B2 优先权日:2019-07-04 标题:Process for the preparation of key intermediates for the synthesis of Eltrombopag or salt thereof 发明人:STABILE PAOLO; SEMERARO FLORIANA 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of Eltrombopag, passing through/using intermediate 5′-Chloro-2′-hydroxy[1,1′-biphenyl]-3-carboxylic acid alkaline metal salt of formula: wherein A is an alkaline metal.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-5231198-A 优先权日:1992-07-06 标题:Asymmetric synthesis of hexahydrodibenzofurans by stereospecific inversion of ortho substituted 2-phenylcyclohexanols 发明人:POWERS MATTEW R; GOLEC FREDERICK A 权利人:RHONE POULENC RORER PHARMA 摘要:This invention relates to the stereospecific process for the preparation, separation and purification of hexahydrodibenzofurans which are used in the preparation of the 5HT 3 compounds. More specifically, the present invention relates to a process for the preparation of substantially optically pure cishexahydrodibenzofuran compounds including at least two chiral fused ring centers which comprises the acidic catalyzed stereospecific ring closure by the intra-molecular inversion of a gamma, i.e. 2', carbon atom of a 2-[(2'-leaving group)cycloalkyl]phenol.
专利号:WO-2013049605-A1 优先权日:2011-09-28 标题 :Processes for the preparation of an intermediate in the synthesis of eltrombopag 发明人:AVDAGIC AMIR; BARAN PHIL S 权利人:ASSIA CHEM IND LTD; TEVA PHARMACEUTICAL USA INC 摘要:3'-Amino-2'-hydroxybiphenyl-3-carboxylic acid (BPCA) and related compounds have been prepared using compounds such as: wherein R 1 is -H, -Cl or -F; R 2 is -Br or -I; and R 3 is -H or -N0 2 . BPCA is useful, for example, in the preparation of Eltrombopag.
专利号:US-2022298116-A1 优先权日:2019-07-04 标题:Process for the preparation of key intermediates for the synthesis of eltrombopag or salt thereof
专利号:WO-9401428-A1 优先权日:1992-07-06 标 题 :Asymmetric synthesis of hexahydrodibenzofurans by stereospecific inversion of ortho substituted 2-phenylcyclohexanols