专利号:US-10751419-B2 优先权日:2014-05-01 标题:Method for synthesis of reactive conjugate clusters 发明人:MIGAWA MICHAEL T; YU JINGHUA; WAN W BRAD; PATEL SAYTEN P; VASQUEZ GUILLERMO; KINBERGER GARTH A; PRAKASH THAZHA P; SETH PUNIT P; SWAYZE ERIC E 权利人:IONIS PHARMACEUTICALS INC 摘要:Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.
专利号:WO-9419366-A1 优先权日:1993-02-26 标题 :Chemical synthesis of squalamine 发明人:MORIARTY ROBERT M; GUO LIANG; TULADHAR SUDERSAN M 权利人:MAGAININ PHARMA 摘要:Methods for the chemical preparation or synthesis of the sterol antibiotic squalamine. Preferably, the preparation is by modifying the 3-position of a 3-oxo-7α-hydroxy-24z-ether protected alcohol group-5α-cholestane with a spermidino moiety to form a 3β-spermidino-7α-hydroxy-24z-ether protected group -5α-cholestane; deprotecting the 24-position of the 3β-spermidino-7α-hydroxy-24z-ether protected group-5α-cholestane to the free hydroxyl; and sulfating the 24-position of the 3β-spermidino-7α, 24-dihydroxy-5α-cholestane.
专利号:US-4134904-A 优先权日:1977-08-30 标 题 :Synthesis of steroids 发明人:KAISER EMIL T 权利人:KAISER EMIL T 摘要:The synthesis of 25-hydroxycholesterol from animal bile starting materials in which hyodeoxychloic acid or an ester thereof is converted to the 3β-hydroxy-5-cholenic acid alkyl ester, and then converted to 3β-hydroxy-25-cyano-5-cholene by a series of steps in which the sterol nucleus is stablized by use of a 3α,5α-bridge sometimes called an i-steroid configuration, and the carbon chain then extended from the carbon at the 24-position to a cyanide group at the 25-position. The compound so formed is subjected to a series of reactions by which it is transformed into 25-hydroxy-7-dehydrocholesterol which may then be irradiated with ultraviolet light to 25-hydroxycholecalciferol. The invention discloses new and improved processes for preparing these end products and also the compounds formed as intermediates and processes for preparing these intermediates.
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-4287129-A 优先权日:1980-07-28 标 题:Synthesis of 1α-hydroxy-7-dehydrosteroids 发明人:KLAUSMEIER WILLIAM H; JOHNSON RICHARD L; HIRSCH ARNOLD L 权利人:DIAMOND SHAMROCK CORP 摘要:Enol acetylation is carried out on a variety of 1,4,6-trien-3-ones to form 1,3,5,7 tetraene structures from which 1 alpha -hydroxy-7-dehydro steroids are obtained. The compounds are intermediates used in the preparation of vitamin D3 metabolites such as 1 alpha ,25-dihydroxyvitamin D3 and 1 alpha -hydroxyvitamin D3.
参考文献:10.1194/jlr.m400157-jlr200 摘要:Mano N, Sato Y, Nagata M, Goto T, Goto J. Bioconversion of 3beta-hydroxy-5-cholenoic acid into chenodeoxycholic acid by rat brain enzyme systems. J Lipid Res. 2004 Sep;45(9):1741–8. doi: 10.1194/jlr.m400157-jlr200.