专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:US-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-7429658-B2 优先权日:2003-09-11 标题 :Synthesis of protected pyrrolobenzodiazepines 发明人:HOWARD PHILIP; MASTERSON LUKE 权利人:SPIROGEN LTD 摘要:A method of synthesis of a N-10 protected PBD compound of formula (I): n nvia an intermediate of formula (II) or formula (V):
专利号:US-9512096-B2 优先权日:2011-12-22 标题 :Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds 发明人:CHEN WEIRONG; HUMORA MICHAEL; KWOK DAW-LONG ALBERT; KIESMAN WILLIAM F; IRDAM ERWIN AYANDRA 权利人:KNOPP BIOSCIENCES LLC; KNOPP BIOSCIENCES LLP 摘要:The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.
专利号:US-7557099-B2 优先权日:2004-03-01 标题 :Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines 发明人:HOWARD PHILIP WILSON; KANG GYOUNG-DONG 权利人:SPIROGEN LTD 摘要:Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R 2 and R 3 are independently selected from —H, â•?O, â•?CH 2 , —CN, —R, OR, halo, â•?CH—R, O—SO 2 —R, CO 2 R and COR; R 10 is a carbamate-based nitrogen protecting group; and R 11 is an oxygen protecting group.