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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Preparation and catalytic evaluation of a palladium catalyst deposited over modified clinoptilolite (Pd&at;MCP) for chemoselective N-formylation and N-acylation of amines
Amirsoleimani, Mina,Khalilzadeh, Mohammad A.,Zareyee, Daryoush
, (2020/08/22)
Novel palladium nanoparticles stabilized by clinoptilolite as a natural inexpensive zeolite prepared and used for N-formylation and N-acylation of amines at room temperature at environmentally benign reaction conditions in good to excellent yields. Pd (II) was immobilized on the surface of clinoptilolite via facile multi-step amine functionalization to obtain a sustainable, recoverable, and highly active nano-catalyst. The structural and morphological characterizations of the catalyst carried out using XRD, FT-IR, BET and TEM techniques. Moreover, the catalyst is easily recovered using simple filtration and reused for 7 consecutive runs without any loss in activity.
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.
