367487-89-6Relevant academic research and scientific papers
Silver/palladium relay catalyzed 1,3-dipole annulation/allylation reactions to access fully substituted allyl imidazolidines
Han, Ruiping,Ding, Yue,Jin, Xueke,Li, Er-Qing
supporting information, p. 646 - 649 (2020/02/11)
A silver/palladium relay catalyzed 1,3-dipole annulation/allylation reaction of iminoesters and Baylis-Hillman acetates for the construction of fully substituted allyl imidazolidines is reported. The reaction of both iminoesters and Baylis-Hillman acetate
On the development of a nucleophilic methylthiolation methodology
Carvalho, Bernardo Basbaum Portinho De Puga,Amaral, Adriane Antonia Pereira,De Castro, Pedro P?ssa,Ferreira, Fernanda Cerqueira Moreira,Horta, Bruno Araújo Cautiero,Amarante, Giovanni Wilson
, p. 5420 - 5426 (2020/08/03)
Methylthiolation reactions are usually explored to access organosulfur compounds using methanethiol, an extremely flammable and toxic compound. Herein, methylthiomethyl esters were successfully applied as novel methylthiolation reagents in a low cost, transition-metal-free methodology. These reagents allowed the methylthiolation of a wide scope of chalcones, acyl ester derivatives and Morita-Baylis-Hillman acetates with good group tolerance, affording the methylthiolated products in moderate to excellent yields. The reaction mechanism was investigated through several control experiments, as well as by theoretical calculations employing Density Functional Theory. The results strongly support that a sulfurane and a sulfonium ylide appear as key intermediates and that a Pummerer type rearrangement is also crucial for the formation of this novel reagent. Furthermore, the methylthiolation mechanism is likely to proceed through the nucleophilic attack of the reagent, followed by an entropically favoured step involving the acetate attack to the positively charged species, then releasing the product. This journal is
Fe(III)-Catalyzed Hydroallylation of Unactivated Alkenes with Morita-Baylis-Hillman Adducts
Qi, Jifeng,Zheng, Jing,Cui, Sunliang
supporting information, p. 1355 - 1358 (2018/03/09)
An Fe(III)-catalyzed hydroallylation of unactivated alkenes with Morita-Baylis-Hillman adducts via an Fe-catalyzed process is described. A variety of alkenes, including mono-, di-, and trisubstituted alkenes, could all smoothly convert to structural diver
PYRIDOPYRIMIDINE BASED DERIVATIVES AS POTENTIAL PHOSPHODIESTERASE 3 (PDE3) INHIBITORS AND A PROCESS FOR THE PREPARATION THEREOF
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Paragraph 0082; 0103; 0104; 0112, (2014/08/19)
The present invention provides compounds of formula 1 as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where
INDOLIZINONE BASED DERIVATIVES AS POTENTIAL PHOSPHODIESTERASE 3 (PDE3) INHIBITORS AND A PROCESS FOR THE PREPARATION THEREOF
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Paragraph 0077, (2014/10/16)
The present invention provides compounds of general formula A useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula A can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases.
Aromatic spiroketal bisphosphine ligands: Palladium-catalyzed asymmetric allylic amination of racemic Morita-Baylis-Hillman adducts
Wang, Xiaoming,Meng, Fanye,Wang, Yan,Han, Zhaobin,Chen, Yong-Jun,Liu, Li,Wang, Zheng,Ding, Kuiling
supporting information, p. 9276 - 9282 (2012/10/29)
Showing a backbone: The spiroketal backbone of the bis(phosphine) ligand 1 led to good regio- and enantioselectivity in the palladium-catalyzed asymmetric allylic amination of racemic Morita-Baylis-Hillman adducts with aromatic amines. The methodology provides a facile and efficient synthesis of precursors for optically active β-lactam derivatives, including the cholesterol drug Ezetimibe.
Synthesis and evaluation of novel 2-pyridone derivatives as inhibitors of phosphodiesterase3 (PDE3): A target for heart failure and platelet aggregation
Ravinder, Mettu,Mahendar, Budde,Mattapally, Saidulu,Hamsini, Kommi Venkata,Reddy, Thatikonda Narendar,Rohit, Chilappa,Srinivas, Kolupula,Banerjee, Sanjay Kumar,Rao, Vaidya Jayathirtha
, p. 6010 - 6015 (2012/11/07)
Twenty-six 2-pyridone derivatives (8a-8z), which are structurally analogous to amrinone and milrinone two important cardiotonic drugs, are synthesized and characterized. The synthesis of 2-pyridone derivatives involves addition, followed by cyclization be
Synthesis of allyl aryl sulfone derivatives from Baylis-Hillman acetates in water
Karnakar, Konkala,Shankar, Jilla,Murthy, Sabbavarapu Narayana,Nageswar, Yadavalli Venkata Durga
body text, p. 875 - 880 (2011/06/27)
Various phenyl and p-tolyl allyl sulfone derivatives were prepared stereoselectively by reacting Baylis-Hillman acetates with sodium 4-R-benzenesulfinate (R=H, Me) in H2O. The reaction was very efficient in providing the corresponding sulfone d
Part 148 in the series "studies on novel synthetic methodologies:" Selective acetylation of alcohols, phenols and amines and selective deprotection of aromatic acetates using silica-supported phosphomolybdic acid
Das, Biswanath,Thirupathi, Ponnaboina,Kumar, Rathod Aravind,Laxminarayana, Keetha
, p. 2677 - 2683 (2008/09/19)
An environmentally friendly silica-supported phosphomolybdic acid was found to be a highly efficient catalyst for the selective acetylation of alcohols, phenols and amines in the absence of any solvent and also for the chemoselective deprotection of aromatic acetates under very mild conditions. This method has been used for the protection of the hydroxy groups as well as for the deprotection of the acetates of several naturally occurring bioactive phenolic compounds. The catalyst can be easily recovered and reused.
Identification of 6-substituted 4-arylsulfonyl-1,4-diazepane-2,5-diones as a novel scaffold for human chymase inhibitors
Tanaka, Taisaku,Muto, Tsuyoshi,Maruoka, Hiroshi,Imajo, Seiichi,Fukami, Harukazu,Tomimori, Yoshiaki,Fukuda, Yoshiaki,Nakatsuka, Takashi
, p. 3431 - 3434 (2008/02/10)
A novel series of 6-substituted 4-sulfonyl-1,4-diazepane-2,5-diones were designed, synthesized and evaluated as human chymase inhibitors. Structure-activity relationship studies led to the identification of a potent inhibitor, (6S)-6-(5-chloro-2-methoxybe
