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:WO-9962854-A1 优先权日:1998-06-01 标 题:Solution phase synthesis of olefins and olefin-derived products 发明人:ORGAN MICHAEL G; DIXON CRAIG E; KALDOR STEPHEN W; SIEGEL MILES G 权利人:LILLY CO ELI; ORGAN MICHAEL G; DIXON CRAIG E; KALDOR STEPHEN W; SIEGEL MILES G 摘要:This invention relates to a process for producing a plurality of olefin compounds of formula (I). The method is ideal for generating libraries of compounds for high throughput screening. The invention also provides a library of above compounds physically separated from one another in a reaction vessel. This library is useful for optimizing the activity of therapeutically useful compounds.
专利号:US-10611739-B2 优先权日:2016-08-16 标题:Process for preparation of lactone derivatives and intermediates thereof 发明人:CHEN PING; PENG SHAOPING; LI YINQIANG; LI DAFENG; DONG XUEJUN 权利人:PHARMARESOURCES SHANGHAI CO LTD 摘要:A novel process for the preparation of lactone derivatives, and intermediates thereof is described. The lactone derivatives are important precursors for the synthesis of anti-hepatitis C virus agents, including sofosbuvir.
专利号:US-5919992-A 优先权日:1996-06-11 标 题:Synthesis of haloalkynol 发明人:KUO DAVID L 权利人:LONZA AG 摘要:The present invention relates to process of halogenating an alkynol having 3 to 20 carbon atoms to produce a compound having the formula: R-C 3BOND (C-CH2)x-OH, wherein R is F, Cl, Br or I and x is 1 to 18. In particular, this invention provides a process for preparing a halopropynyl alcohol, specifically iodopropynyl alcohol. In one embodiment, iodopropynyl alcohol is produced by sequentially adding potassium hydroxide, potassium iodide and an oxidizing agent to a solution of propynyl alcohol at a rate and temperature sufficient to produce an iodopropynyl alcohol.
专利号:US-6657066-B1 优先权日:2002-12-10 标题 :Synthesis of certain triazole compounds 发明人:PLACE ILEANA; HARDER JOHN W; ROMANET ROBERT F; VREELAND WILLIAM B 权利人:EASTMAN KODAK CO 摘要:Disclosed is a process for forming a 1H-pyrazolo (1,5-b)-[1,2,4]-triazole compound by ring closing a pyrazoloamidine compound comprising reacting the amidine with an oxidizing agent having a reduction potential vs Ag/AgCl that is more positive than -0.16V and less than +1.43V in the presence of a halogen atom. The invention also discloses certain triazole compounds that are successfully made by the conventional process. The process and compounds of the invention provide improved yields and reduce or eliminate unwanted side-reactions.
专利号:US-7125906-B2 优先权日:2002-04-03 标题 :Indole derivatives having anti-angiogenetic activity 发明人:ARNOULD JEAN-CLAUDE 权利人:ASTRAZENECA AB 摘要:The invention relates to the use of a compound of Formula (I), for the manufacture of a medicament to inhibit and/or reverse and/or alleviate symptoms of angiogenesis and/or any disease state associated with angiogenesis: n nwherein: X, p, q, R 1 , R 2 , R 3 , R 4 , and R 5 are as defined in the description. The invention also related to use of compounds of Formula (I) as medicaments and also to novel compounds of Formula (I). The invention further provides pharmaceutical compositions of compounds of Formula (I) and processes for the synthesis of compounds of Formula (I).
摘要:US EPA; Chemical Data Reporting (CDR). Non-confidential 2012 Chemical Data Reporting information on chemical production and use in the United States. Available from, as of Nov 15, 2014: 摘要:EPA; Pesticide Product Label System (PPLS) - Search for HALOBROM, company no. 8622; product no.25 . Approval date September 17, 2002. Database Available from, as of June 21, 2007: 摘要:US EPA; Non-confidential Production Volume Information Submitted by Companies for Chemicals Under the 1986-2002 Inventory Update Rule (IUR). 2,4-Imidazolidinedione, 1-bromo-3-chloro-5,5-dimethyl- (16079-88-2). Available from, as of February 16, 2007: 摘要:EnviroTech; BCDMH Tabs, Water Treatment Biocide. Modesto, CA: EnviroTech. Available from, as of Nov 14, 2014: 摘要:Franke C et al; Chemosphere 29: 1501-14 (1994)