36646-70-5Relevant academic research and scientific papers
Cu catalyzed cross-dehydrogenative coupling reaction for the synthesis of 3-hydroxy-2-pyrrolidinones
Sarkar, Rajib,Mukhopadhyay, Chhanda
supporting information, p. 3069 - 3076 (2018/07/06)
A new convenient strategy for the synthesis of 3-hydroxy-2-pyrrolidinone derivatives featuring regioselective C–C coupling has been developed. This is a Cu (II) catalyzed cross dehydrogenative coupling (CDC) involving enamino-ketones of benzyl amines and di-alkyl acetylenedicarboxylate, followed by cyclization by primary amines. TBHP (tert-butyl hydroperoxide) has been used as the oxidant to promote the coupling protocol. This synthetic route principally demonstrates the scope of CDC reaction and also applicable to gram-scale synthesis.
Synthetic access to poly-substituted 11H-pyrido[3,2-a]carbazoles, A dna-intercalating ellipticine related structure, and their antiproliferative activity
Wu, Ming-Yu,Shaban, Elkhabiry,Switalska, Marta,Wang, Ning,Shimoda, Miho,Mizutani, Yusuke,Yoshida, Megumi,Mei, Zhen-Wu,Kawafuchi, Hiroyuki,Nokami, Junzo,Wietrzyk, Joanna,Yu, Xiao-Qi,Inokuchi, Tsutomu
, p. 1427 - 1440 (2014/07/07)
The facile procedure for the synthesis of the 11H-pyrido[3,2-a]carbazole structure involving the Fischer indole cyclization on tetrahydroquinolinones, available from enaminones and methyl 2-formyl-3-oxopropanoate, followed by the aromatization of the resulting 5,6-dihydro derivatives is described. This method allows for the introduction of substituents at C2, C6, and C8 to the scaffold by choice of the starting materials. In the biological testing, introduction of the phenyl group at C6 is significantly effective to improve the antiproliferative activity.
Novel, non-acylguanidine-type Na+/H+ exchanger inhibitors: Synthesis and pharmacology of 5-tetrahydroquinolinylidene aminoguanidine derivatives
Fukumoto, Shoji,Imamiya, Eiko,Kusumoto, Keiji,Fujiwara, Shuji,Watanabe, Toshifumi,Shiraishi, Mitsuru
, p. 3009 - 3021 (2007/10/03)
In the course of our research into new types of non-acylguanidine Na+/H+ exchanger (NHE) inhibitors, we designed and synthesized aryl-fused tetrahydropyranylidene and cyclohexylidene aminoguanidine derivatives I (X = O, CH2), which were tested for their inhibitory effects on rat platelet NHEs. After optimization, we found that the S isomer of tetrahydroquinoline derivatives that possess a methyl group in the 4-position and a halogen or methyl group in the o-position of Ar2 exhibited high inhibitory activity. In these compounds, (5E,7S)-[[7-(5-fluoro-2-methylphenyl)-4-methyl-7,8-dihydro-5(6H) -quinolinylidene]amino]guanidine dimethane-sulfonate (18, T-162559) was found to be a potent inhibitor of both rat and human platelet NHEs, with IC50 values of 14 and 13 nM, respectively. Furthermore, in a rat myocardial infarction model in vivo (1 h ischemia-24 h reperfusion), 18 (0.1 mg/kg, intravenously administered 5 min or 2 h before coronary occlusion) showed significant activity (33% or 23% inhibition, respectively). These results suggested that 18 may exhibit a potent and long-lasting protective activity against cardiac injuries induced by ischemia-reperfusion.
Aminoguanidine hydrazone derivatives, process for producing the same and drugs thereof
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Page column 58, (2010/11/29)
The present invention is to provide a compound of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic heterocyclic ring, the ring B an optionally substituted 5- to 6-membered aromatic homocyclic ring or an optionally sub
