专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
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-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.
专利号:US-10155772-B2 优先权日:2010-07-08 标题:Process for the synthesis of substituted morphinans 发明人:DUNCAN SCOTT 权利人:ALKERMES PHARMA IRELAND LTD 摘要:The invention further relates to a process for the synthesis of 3-carboxamide substituted morphinans where a 3-cyano substituted 6-oxo substituted morphinan is reacted with a 1,3-diol.
专利号:US-9006425-B2 优先权日:2009-03-18 标题:Aluminum complexes and their use in the synthesis of cyclic carbonates 发明人:NORTH MICHAEL 权利人:NORTH MICHAEL; UNIV YORK 摘要:Dimeric aluminum catalysts of formula I: and their use in catalyzing the synthesis of cyclic carbonates from epoxides and carbon dioxide.
专利号:US-9029543-B2 优先权日:2011-04-05 标 题:Process for the synthesis of quaternary amine compounds 发明人:DUNCAN SCOTT 权利人:DUNCAN SCOTT; ALKERMES INC 摘要:The invention relates to a process for the synthesis of quaternized compounds of formula: