7500-37-0Relevant articles and documents
Influence of Steric Effect on the Pseudo-Multicomponent Synthesis of N-Aroylmethyl-4-Arylimidazoles
Elejalde-Cadena, Nerith Rocio,García-Olave, Mayra,Figueroa, David,Vidossich, Pietro,Miscione, Gian Pietro,Portilla, Jaime
, (2022/02/19)
A pseudo-three-component synthesis of N-aroylmethylimidazoles 3 with three new C–N bonds formed regioselectively under microwave conditions was developed. Products were obtained by reacting two equivalents of aroylmethyl bromide (ArCOCH2 Br, 1) with the appropriate amidine salt (RCN2 H3.HX, 2) and with K2 CO3 as a base in acetonitrile. The bicomponent reaction also occurred, giving the expected 4(5)-aryl-1H-imidazoles 4. Notably, the ratio of products 3 and 4 is governed by steric factors of the amidine 2 (i.e., R = H, CH3, Ph). Therefore, a computational study was carried out to understand the reaction course regarding product ratio (3/4), regioselectivity, and the steric effects of the amidine substituent group.
Metal-Free Amidation Reactions of Terminal Alkynes with Benzenesulfonamide
Mahato, Sachinta,Santra, Sougata,Zyryanov, Grigory V.,Majee, Adinath
, (2019/03/19)
A novel and efficient approach has been developed to synthesize α-sulfonylamino ketones through the reaction between terminal alkynes and sulfonamides under ambient air using PIDA (diacetoxy iodobenzene). A library of α-sulfonylamino ketone derivatives having a variety of substituents has been synthesized. A plausible reaction pathway has been predicted. This reaction offers a broad substrate scope, metal-free synthesis, excellent regioselectivity, easily accessible reactants, and room temperature reaction conditions under ambient air and is operationally simple. A gram-scale synthesis demonstrates the potential applications of the present method. In addition, we have also synthesized α-acetoxy ketones in the case of absence of sulfonamide.
Amino propylene glycol derivatives, its preparation method and its pharmaceutical composition and use thereof
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Paragraph 0174; 0177; 0178; 0179, (2018/11/22)
The invention discloses a class of amino propanediol derivatives, a preparation method, drug compositions and uses thereof, and particularly relates to a class of new immunoloregulation agents represented by a general formula (I), a preparation method, drug compositions containing the immunoloregulation agents, and especially uses of the immunoloregulation agents as immunoloregulation drugs. The compound with characteristics of excellent treatment effect and low toxicity can be used in the fields of immunologic derangement and immunosuppression, and can further be used for treatment of hypoimmunity, organ transplant rejection and autoimmune diseases. The formula I is defined in the instruction.