16078-30-1Relevant articles and documents
Mild Rh(III)-catalyzed C7-allylation of indolines with allylic carbonates
Park, Jihye,Mishra, Neeraj Kumar,Sharma, Satyasheel,Han, Sangil,Shin, Youngmi,Jeong, Taejoo,Oh, Joa Sub,Kwak, Jong Hwan,Jung, Young Hoon,Kim, In Su
, p. 1818 - 1827 (2015)
The rhodium(III)-catalyzed direct allylation of indolines with allylic carbonates at room temperature is described. These transformations provide the facile and efficient construction of C7-allylated indolic scaffold.
A rapid and clean synthetic approach to cyclic peptides: Via micro-flow peptide chain elongation and photochemical cyclization: Synthesis of a cyclic RGD peptide
Mifune, Yuto,Nakamura, Hiroyuki,Fuse, Shinichiro
, p. 11244 - 11249 (2016)
A cyclic RGD peptide was efficiently synthesized based on micro-flow, triphosgene-mediated peptide chain elongation and micro-flow photochemical macrolactamization. Our approach enabled a rapid (amidation for peptide chain elongation 5 s, macrolactamization 5 min) and clean (only one column chromatographic separation) synthesis of a cyclic peptide.
Cobalt Catalyzed Hydroarylation of Michael Acceptors with Indolines Directed by a Weakly Coordinating Functional Group
Banjare, Shyam Kumar,Chebolu, Rajesh,Ravikumar
, p. 4049 - 4053 (2019)
A cobalt(III) catalyzed hydroarylation of Michael acceptors using indolines, selectively at the C-7 position, has been reported. For the selective C-7 functionalization of indoline, we have used a weakly coordinating amide carbonyl group. During the process of optimization, we have also discovered the unusual cocatalytic activity of zinc triflate in the C-H functionalization reaction. Hydroarylation of unprotected maleimide using indolines was a challenging substrate and never accomplished before, we were able to achieve this with our methodology in good yields.
A New Method for Preparation of 2-Aminopyridine:Borane and its Analogues
Okamoto, Yoshihisa,Osawa, Toshimitsu,Kinoshita, Toshio
, p. 462 - 464 (1982)
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Method for promoting acylation of amine or alcohol by carbon dioxide
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Paragraph 0033-0034, (2021/05/29)
The invention relates to a method for promoting acylation of amine or alcohol by carbon dioxide, which comprises the following steps of: mixing an amine compound, carboxylate or thiocarboxylate compound and a reaction solvent under the action of carbon dioxide, and reacting to obtain an amide compound, or under the action of carbon dioxide, mixing the alcohol compound, the thiocarboxylate compound and the reaction solvent [gamma]-valerolactone, and reacting to obtain the ester compound. According to the invention, under the promotion action of carbon dioxide, carboxylate or thiocarboxylate is used as an acylation reagent, and amine and alcohol are converted into amide and ester compounds in the absence of a transition metal catalyst, so that acylation reagents such as acyl chloride or anhydride with irritation and corrosivity are avoided; and the method has the advantages of simple operation, mild reaction conditions, high tolerance of substrate functional groups, strong applicability and high yield, and provides an efficient, reliable and economical preparation method for synthesis of amide and ester compounds.
Efficient synthesis process of medical intermediate 5-bromoindole
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Paragraph 0036-0037; 0039; 0043-0044; 0046; 0050-0051; 0053, (2020/08/06)
The invention discloses an efficient synthesis process of a medical intermediate 5-bromoindole, comprising the following steps of: using an indole compound as a raw material, carrying out low-pressureliquid-phase hydrogenation to destroy five-membered ring conjugation of indole to obtain an indoline compound; enabling the indoline compound to react with an acylation reagent, and protecting nitrogen, so as to obtain an N-acyl indoline compound; carrying out bromination on the N-acyl indoline compound to obtain a 5-bromo-N-acyl indoline compound; carrying out deacylation protection on the 5-bromo-N-acyl indoline compound to obtain a 5-bromoindoline compound; and carrying out oxidative dehydrogenation on the 5-bromoindoline compound by using oxygen or air under the action of a cuprous catalyst and nitric oxide to obtain the target compound 5-bromoindole. The steps involved in the process are convenient to operate, the conditions are mild, and environmental pollution is reduced; finally,the prepared product is high in yield, high in purity and low in energy consumption.