Transition-Metal-Free Regioselective Construction of Diverse 3-Carbonyl Functionalized 4-Pyrones<i>via</i>Thermal Wolff-Rearrangement of Diazodicarbonyls
作者:Ga Eul Park、Shizuka Mei Bautista Maezono、Ji Hyeon Ha、Jae-Jin Shim、Sung Hong Kim、Yong Rok Lee
DOI:10.1002/adsc.201800874
日期:2018.12.3
An efficient protocol for the construction of 3‐carbonyl functionalized 4‐pyrones has been developed using a transition‐metal free thermal cascade reaction of diazodicarbonyls with β‐enamino esters or β‐enamino ketones. This reaction proceeds via cascade carbene generation, ketene formation via thermal Wolff‐rearrangement, nucleophilic addition, intramolecular cyclization, and elimination. This protocol
利用重氮二羰基与β-烯胺酸酯或β-烯胺酮的无过渡金属热级联反应,开发了一种有效的构建3-羰基官能化的4-吡喃酮的方法。该反应通过级联卡宾生成,通过热Wolff重排形成烯酮,亲核加成,分子内环化和消除而进行。该协议为各种2,3,5-三取代的4-吡喃酮衍生物提供了快速的合成途径。
[EN] PROCESS FOR THE PREPARATION OF 1-METHYL-6-[6-R2-5-METHYL-8-(METHYLAMINO)-4-[ (3AS,6AS)-5-METHYL-2,3,3A,4,6,6A-HEXAHYDROPYRROLO[2,3-C]PYRROL-1-YL]-9H-PYRIDO[2,3-B]INDOL-3-YL]-4-OXO-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID HYDROCHLORIDE<br/>[FR] PROCÉDÉ DE PRÉPARATION DE CHLORHYDRATE D'ACIDE 1-MÉTHYL-6-[6-R2-5-MÉTHYL-8-(MÉTHYLAMINO)-4-[(3 AS, 6 AS)-5-MÉTHYL -2,3,3 A,4,6,6 A-HEXAHYDROPYRROLO[2,3-C]PYRROL-1-YL]-9 H-PYRIDO[2,3-B]INDOL-3-YL]-4-OXO-1,8-NAPHTYRIDINE-3-CARBOXYLIQUE
申请人:HOFFMANN LA ROCHE
公开号:WO2022078923A1
公开(公告)日:2022-04-21
The present invention relates to a process for synthesizing a compound of formula (I), wherein R1is hydrogen or halogen; R2is hydrogen, halogen or cyano; n is 0-7, particularly n is 2-3, more particularly n is 2; or diastereomer, pharmaceutically acceptable salts thereof, which is useful for prophylaxis and treatment of a disease caused by bacteria infection.
本发明涉及一种合成式(I)化合物的方法,其中R1为氢或卤素;R2为氢、卤素或氰基;n为0-7,特别是n为2-3,更特别是n为2;或其对映异构体、药学上可接受的盐,用于预防和治疗由细菌感染引起的疾病。
Guemas, Jean-Pierre; Lees, Michele; Reliquet, Alain, Phosphorus and Sulfur and the Related Elements, 1981, vol. 12, p. 325 - 340
作者:Guemas, Jean-Pierre、Lees, Michele、Reliquet, Alain、Villieras, Jean
DOI:——
日期:——