90481-68-8Relevant academic research and scientific papers
Pd-tBuONO Cocatalyzed Aerobic Indole Synthesis
Ning, Xiao-Shan,Liang, Xin,Hu, Kang-Fei,Yao, Chuan-Zhi,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 1590 - 1594 (2018/04/30)
A Pd-tBuONO co-catalyzed scalable and practical synthesis of indoles with molecular oxygen as terminal oxidant is developed. Either terminal or internal 2-vinylanilines could be smoothly converted to desired indoles under one general condition. This method has been evaluated in the large scale synthesis of indomethacin and a potential anti-breast cancer drug candidate 1. (Figure presented.).
Chemoselectivity in the Kosugi-Migita-Stille coupling of bromophenyl triflates and bromo-nitrophenyl triflates with (ethenyl)tributyltin
Ansari, Nurul N.,Cummings, Matthew M.,S?derberg, Bj?rn C.G.
, p. 2547 - 2560 (2018/04/20)
Kosugi-Migita-Stille cross coupling reactions of (ethenyl)tributyltin with all isomeric permutations of bromophenyl triflate and bromo-nitrophenyl triflate were examined in order to determine the chemoselectivity of carbon-bromine versus carbon-triflate bond coupling under different reaction conditions. In general, highly selective carbon-bromine bond cross couplings were observed using for example bis(triphenylphosphine)palladium dichloride (2 mol-%) in 1,4-dioxane at reflux. In contrast, reactions using the same pre-catalyst but in the presence of a three-fold excess of lithium chloride in N,N-dimethylformamide at ambient temperature were in most cases selective for coupling at the carbon-triflate bond. Overall, isolated yields and the selectivity for carbon-bromine bond coupling were significantly higher compared to carbon-triflate bond coupling.
HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
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Page/Page column 76, (2016/05/19)
The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and may be useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
A new method for the synthesis of 2,6-dinitro and 2-halo-6-nitrostyrenes
Mundla
, p. 6319 - 6321 (2007/10/03)
A new method for the synthesis of 2-halo-6-nitrostyrenes from 2-halo-6-nitrotoluenes is disclosed. Also described is a one-pot process for the synthesis of 2,6-dinitristyrene from 2,6-dinitrotoluene. (C) 2000 Elsevier Science Ltd.
Palladium-Catalyzed Reactions in the Synthesis of 3- and 4-Substituted Indoles. Approaches to Ergot Alkaloids
Harrington, Peter J.,Hegedus, Louis S.
, p. 2658 - 2662 (2007/10/02)
An efficient synthesis of 4-bromo-1-tosylindole (10) based on the Pd(II)-catalyzed cyclization of an o-ethenylaniline p-toluenesulfonamide has been developed.A Pd(0) oxidative addition-olefin insertion-β-hydride elimination cycle converted 10 to a number of 4-substituted 1-tosylindoles.Selective electrophilic substitutions at the 3-position of 10 provided access to the 3-(chloromercurio)- (18) and 3-iodo-1-tosylindoles (22).Transmetalation to palladium and allyl chloride insertion converted 18 to 3-allyl-4-bromo-1-tosylindole (20) which could be cyclized to the benzindoline 21.A Pd(0) oxidative addition-olefin insertion-β-hydride elimination cycle converted the 3-iodo compound 22 to a number of 4-bromo-3-substituted 1-tosylindoles including 24, a potential precursor to optically active tryptophans.
