101286-71-9Relevant academic research and scientific papers
Atom-efficient transition-metal-free arylation ofN,O-acetals using diarylzinc reagents through Zn/Zn cooperativity
Borys, Andryj M.,Gil-Negrete, Jose M.,Hevia, Eva
supporting information, p. 8905 - 8908 (2021/09/10)
Exploiting the cooperative action of Lewis acid Zn(C6F5)2with diarylzinc reagents, the efficient arylation ofN,O-acetals to access diarylmethylamines is reported. Reactions take place under mild reaction conditions without the need for transtion-metal catalysis. Mechanistic investigations have revealed that Zn(C6F5)2not only acts as a Lewis acid activator, but also enables the regeneration of nucleophilic ZnAr2species, allowing a limiting 50 mol% to be employed.
Copper(I)-catalyzed coupling reaction of aryl boronic acids with N,O-acetals and N,N-aminals under atmosphere leading to α-aryl glycine derivatives and diarylmethylamine derivatives
Sakai, Norio,Hori, Hiroaki,Yoshida, Yoshihiro,Konakahara, Takeo,Ogiwara, Yohei
, p. 4722 - 4729 (2015/07/27)
We demonstrated a copper(I)-catalyzed coupling reaction of aryl boronic acids with N,O-acetals and N,N-aminals leading to the synthesis of α-aryl glycines and diarylmethylamines. Under an ambient atmosphere, this catalytic system could be applied to the activation of a C(sp3)-O bond of N,O-acetals with an ester and an aryl group, or without a coordinating substituent, as well as to a C(sp3)-N bond of N,N-aminals.
Synthesis and insulin-sensitizing activity of (S)-2-ethoxy-3- phenylpropanoic acid derivatives
Cai, Xiao-Hua,Xie, Bing
, p. 1106 - 1109 (2007/10/03)
A series of (S)-2-ethoxy-3-phenylpropanoic acid derivatives were synthesized and their insulin-sensitizing activities were evaluated in 3T3-L1 cells. Compounds 1b (EC30 = 9.43 × 10-3 μmol/L), 1d (EC30 = 7.45 × 10-3 μmol/L), 1e (EC 30 = 6.22 × 10-3 μmol/L), and 1f (EC30 = 7.76 × 10-3 μmol/L) exhibited more potent insulin-sensitizing activity than rosiglitazone (EC30 = 2.06 × 10-2 μmol/L).
Synthesis and evaluation of methyl 2-methoxycarbonyl-3-phenylpropionate derivatives as a new type of angiotensin converting enzyme inhibitors
Cai, Xiao-Hua,Xie, Bing,Guo, Hui
, p. 1110 - 1113 (2007/10/03)
Methyl 2-methoxycarbonyl-3-phenylpropionate derivatives were prepared, and their inhibitory activities for angiotensin converting enzyme (ACE) were evaluated. Compounds 5b (IC50 = 0.0039 μmol/L), 5d (IC 50 = 0.0027 μmol/L), 5e (IC50 = 0.0021 μmol/L), and 5f (IC50 = 0.0052 μmol/L) exhibited more potent ACE inhibitiory activity than the control drug Captopril (IC50 = 0.0075 μmol/L).
3-piperidyl-4-oxoquinazoline derivatives and pharmaceutical compositions comprising the same
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, (2008/06/13)
3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3and R4independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.
Reductive Cleavage of N-Substituted 2-Aryl-1,3-oxazolidines: Generation of α-Amino-Substituted Carbanions
Azzena, Ugo,Melloni, Giovanni,Nigra, Cristina
, p. 6707 - 6711 (2007/10/02)
The behavior of several N-substituted 2-aryl-1,3-oxazolidines has been investigated under conditions of electron transfer from alkali metals in aprotic solvents.The reduction led to the regioselective cleavage of the benzylic carbon-oxygen bond, with formation of the corresponding N-substituted benzylamino alcohols in good yields.Investigation of the mechanism of this reductive cleavage, with the aid of labeling experiments, showed the intermediate formation of α-tertiary amino-substituted carbanions.
