CAS: 5548-10-7; Indole-3-Glyoxylamide

上下游产品

indolyl-3-glyoxylyl chloride 2-(3-indolyl)oxoacetic acid methyl ester indole oxalyl dichloride2-(1-methyl-1H-indol-3-yl)-2-oxoacetamide tryptamine N,N-dimethyl-1-(2'-bromobenzoyl)tryptamine

吲哚-3-乙腈置于氧气,Copper Diacetate,乙酰氯体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,80.0 °C,101.33 Kpa 条件下,反应 6.0H,反应生成 2-乙酰氨基-1,2,5-三脱氧-1,5-亚氨基-D-葡萄糖醇
参考文献:铜(II)介导的苯甲酰亚胺酯的有氧氧化:初级α-酮酰胺的合成
标题:铜(II)介导的苯甲酰亚胺酯的有氧氧化:初级α-酮酰胺的合成
摘要:已经发现一种简单直接的合成伯α-酮酰胺的方法.该反应代表了通过使用可持续的分子氧作为氧化剂将亚氨基苄基酯直接转化为伯α-酮酰胺的第一个例子.该反应在铜盐(II)的存在下通过裂解亚氨酸苄基的苄基c-h和c-o键进行,唯一的副产物是醇的释放.广泛的底物范围,操作温和的条件,使用单个底物以及放大至克数的反应,使得该策略非常具有吸引力和实用性.此外,机理研究表明,与苄基位置相邻的亚氨酸酯基团在促进该化学过程中起着至关重要的作用.
DOI:10.1021/acs.Joc.6B01262

专利信息

专利号:US-7241900-B2
优先权日:2002-02-12
标题 :Synthesis of indole thiazole compounds as ligands for the Ah receptor
发明人：DELUCA HECTOR F; GRZYWACZ PAWEL K; SICINSKI RAFAL R
权利人:WISCONSIN ALUMNI RES FOUND
摘要:A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.

专利号:US-10081610-B2
优先权日:2014-09-12
标题 :Efficient and scalable synthesis of 2-(1′h-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester and its structural analogs
发明人：SONG JIASHENG; ZHANG SUOMING; LI GUODONG; YANG LUQUING
权利人:ARIAGEN INC
摘要:Methods of synthesizing 2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) and structural analogs thereof. The methods include condensation reactions or condensation and oxidation reactions to form the thiazoline or thiazole moiety of ITE or its structural analogs.

专利号:WO-0144184-A1
优先权日:1999-12-16
标题:Synthesis of indole-containing spla2 inhibitors
发明人：MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT
权利人:LILLY CO ELI; MARTINELLI MICHAEL JOHN; SAWYER JASON SCOTT
摘要:A method of making a compound include reacting a compound represented by formula (I), with a base, to form the compound of formula (II); and where R1 is H, R10 or -C(O)R10; R2 is R20 -OR20, -SR20, -NR20R20' or -C(O)R20;R3, R4, R5, R6 and R7 are each individually H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R or -S(O)2R; provided that at least one of R4 and R5 is not H; each R, R10 and R20 is individually alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; each R' and R20' is individually H, alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; and W is a trisubstituted phosphorous. The method provides an alternative route to indole-3-glyoxylamide compounds.

专利号:WO-0144185-A1
优先权日:1999-12-16
标题 :Carbon monoxide-based synthesis of spla2 inhibitors
发明人：SAWYER JASON SCOTT
权利人:LILLY CO ELI; SAWYER JASON SCOTT
摘要:A method of making a compound, comprises reacting a compound represented by formula (I), with CO and a catalyst, to form the compound of formula (II); where formula (I) is and, formula (II) is and where R2 is selected from the group consisting of R20 -OR20, -SR20, -NR20R20'and -C(O)R20; R3, R4, R5, R6 and R7 are each individually selected from the group consisting of H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R and -S(O)2R; provided that at least one of R4 and R5 is not H; each R and R20 is individually selected from the group consisting of alkyl, alkenyl, alkynyl, aryl and heterocyclic radical; and each R' and R20' is individually selected from the group consisting of H, alkyl, alkenyl, alkynyl, aryl and heterocyclic radical. The method provides an alternative route to indole-3-glyoxylamide compounds.

专利号:US-2004204588-A1
优先权日:2002-02-12
标题 :Synthesis of indole thiazole compounds as ligands for the Ah receptor

专利号:EP-1480951-A1
优先权日:2002-02-12
标题:Synthesis of indole thiazole compounds as ligands for the ah receptor