Synthesis of 1-Amino-2,2,2-trifluoroalkylphosphonates from Alkene-Tethered Trifluoroacetimidoyl Chlorides
作者:José F. Rodríguez、Anji Zhang、Ramon Arora、Mark Lautens
DOI:10.1021/acs.orglett.1c02750
日期:2021.10.1
The reaction of alkene-tethered trifluoroacetimidoylchlorides with trialkylphosphites furnishes 1-amino-2,2,2-trifluoroalkylphosphonates. The products were generated in moderate to good yields, and the scalability of this process was showcased. Partial hydrolysis of the phosphonate moiety was achieved. The cyclization is proposed to occur via formation of an imidoyl phosphonate intermediate that
Synthesis of Diiodinated All-Carbon 3,3′-Diphenyl-1,1′-spirobiindene Derivatives via Cascade Enyne Cyclization and Electrophilic Aromatic Substitution
作者:Quanzhe Li、Liuzhu Yu、Yin Wei、Min Shi
DOI:10.1021/acs.joc.9b01418
日期:2019.7.19
from the reaction of propargyl alcohol-tethered alkylidenecyclopropanes with iodine. The reaction proceeded through an iodination-initiated cascade intramolecular enyne cyclization and electrophilic aromatic substitution reaction process in 1,2-dichloroethane upon heating, giving desired spirocyclic products in moderate to excellent yields. Further transformation of the obtained products has also been
Nickel-Catalyzed Synthesis of Benzo[<i>b</i>]naphtho[1,2-<i>d</i>]azepine via Intramolecular Radical Tandem Cyclization of Alkyl Bromide-Tethered Alkylidenecyclopropanes
作者:Bo Jiang、Jia-Xin Liu、Yin Wei、Min Shi
DOI:10.1021/acs.orglett.8b02699
日期:2018.10.5
A Ni(II)-catalyzed tandem cyclopropane ring opening and radical alkylation of the aromatic ring using unactivated alkyl bromide-tethered alkylidenecyclopropanes (ACPs) have been described in this paper. This ring-forming process exhibits a broad substrate scope with a variety of primary alkyl bromides and aromatic rings, affording diversified benzo[b]naphtho[1,2-d]azepine derivatives in moderate-to-excellent
本文描述了Ni(II)催化的串联环丙烷丙烷开环和使用未活化的烷基溴-束缚的亚烷基环丙烷(ACP)对芳环进行自由基烷基化。这种成环过程显示出具有多种伯烷基溴和芳族环的广泛底物范围,在温和条件下以中等至优异的产率提供了多种苯并[ b ]萘[1,2- d ] a庚因衍生物。在包括氘标记检查在内的几个对照实验的基础上,提出了合理的反应机理。还对获得的多环产物进行了进一步的衍生化。
Electrochemical intramolecular N(sp<sup>2</sup>)–H/N(sp<sup>3</sup>)–H coupling for the synthesis of 1<i>H</i>-indazoles
作者:Qiang Zhong、Pei-Long Wang、Hui Gao、Fang Ma、Youqing Yang、Hongji Li
DOI:10.1039/d3gc00380a
日期:——
The electrochemical synthesis of 1H-indazoles via an intramolecular N(sp2)–H/N(sp3)–H coupling reaction at room temperature is first described. The transition metal-free electrochemical cyclization features the use of commercially available NH3 as the nitrogen source and a broad substrate scope, thus affording a wide range of substituted 1H-indazoles in moderate to good yields. Both the control experiments
Phenyl substituted pyrido(1,4)benzodiazepines and intermediates therefor
申请人:A.H. ROBINS COMPANY, INCORPORATED
公开号:EP0076017A2
公开(公告)日:1983-04-06
[2-[(Aminopyridinyl)amino]Phenyl]aryl-methanones which also have antidepressant activity are used to prepare pyrido[1,4]benzodiazepines having antidepressant activity of the formula
wherein Ar is 2, 3 and 4-pyridinyl, 2 or 3-thienyl, phenyl or a substituted phenyl; R is hydrogen, loweralkyl or an amine on the end of a hydrocarbon chain; Z is hydrogen, halogen, trifluoromethyl, loweralkyl, loweralkoxy, hydroxy or nitro; and Y is hydrogen, loweralkyl, loweralkoxy or hydroxy; and the pharmaceutical salts thereof.