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A conceptually distinct strategy enabling malonylamination of alkenes with abundant amines and iodonium ylides without assistance of any transition metal was developed. Succinimide was identified as a proton shuttle that can not only largely accelerate the process of trapping highly unstable radical ion pairs with alkenes but also significantly improve the chemical yields.

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[Figure not available: see fulltext.] The morpholine (1,4-oxazinane) motif attracted significant attention due to its widespread availability in natural products and biologically relevant compounds. This review describes recent advances in the synthesis of morpholines and their carbonyl-containing analogs from 1,2-amino alcohols, aziridines, epoxides, and related compounds. Special attention is paid to the syntheses performed in a stereoselective manner and using transition metal catalysis. Selected works published since 2013 are covered.

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(Chemical Equation Presented) A systematic investigation of the reductive ring-expansion reaction of cyclic ketoximes fused to aromatic ringswith diisobutylaluminum hydride (DIBALH) is described. This reaction regioselectively afforded a variety of five- to eight-membered bicyclic heterocycles or tricyclic heterocycles containing nitrogen neighboring an aromatic ring, including indoline, 1,2,3,4,5,6-hexahydrobenz[b]azocine, 3,4-dihydro-2H-benzo[b] [1,4]oxazine, 2,3,4,5-tetrahydrobenzo[b][1,4]thiazepine, 1,2,3,4,5,6- hexahydroazepino[3,2-b]-indole, 2,3,4,5-tetrahydro-1H-benzothieno[2,3-b]azepine, 2,3,4,5-tetrahydro-1H-benzothieno[3,2-b]-azepine, 5,6-dihydrophenanthridine, and 5,6,11,12-tetrahydrodibenz[b, f]azocine. The reaction mechanism leading to the rearrangement was investigated on the basis of the restricted Becke three-parameter plus Lee-Yang-Parr (B3LYP) density functional theory (DFT) with the 6-31G (d) basis set. It was found that the reaction proceeds through a three-centered transition state via a stepwise mechanism because the potential energy curve along the intrinsic reaction coordinate (IRC) had twomaxima (saddle points; TS1 and TS2) and the partial phenonium cation intermediate C. In addition to cyclic ketoximes fused to aromatic rings, the reactions of various cyclic and acyclic ketoximeswere examined to investigate preference of migrating group. It was found that themore electron-rich group migrated preferentially to give the corresponding secondary amines.

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A new regioselective method for the synthesis of multifunctionalized indoles from [3 + 2] annulation of 2-bromocyclopropenes with anilines has been developed. By employing a nickel complex as a catalyst, 27 examples of indole products were obtained in good yields with excellent regioselectivity. Synthetic utility of the resulting product was demonstrated in a concise synthesis of biologically active compound Paullone.

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An optimised method for preparing a fuel additive f is provided. The method comprises carrying out the following reaction: (c, d, e) Starting material c may be prepared using an optimised method which comprises carrying out the following reaction: (a, b, c)

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Compounds of the formula: STR1 where 2 THE R’s are the same or different and are H or CH3, and one of them can be C2 -C9 alkyl or phenyl; R1 is hydrogen, C1 -C4 alkyl, C3 -C6 cycloalkyl, C2l -C4 alkoxycarbonyl, or substituted C1 -C4 alkyl where the substituent is C3 -C6 cycloalkyl or phenyl; and Z is H, Cl or CH3 ; and their pharmaceutically suitable salts. The compounds are useful as sedatives; some of them also exhibit antidepressant activity.

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A method is provided for preparing a fuel additive having the formula: ( l ) The method comprises carrying out the following reactions: (i) addition of an alkylating agent b to starting material a: (a) to form an intermediate c; and (ii) ring closing intermediate c to form fuel additive e.

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The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

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A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.

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A palladium-catalyzed multicomponent reaction (MCR) involving aryne, CO, and aniline is established for straightforward assembly of a phenanthridinone scaffold through C-H bond activation. Free combination with multiple kinds of readily available anilines and arynes is facilely achieved for phenanthridinone construction without prefunctionalization. Representative natural products were subsequently synthesized through this MCR strategy highly efficiently. Control experiments and interval NMR tracking revealed the mechanism, particularly the key role of CuF2 in determining the aryne-releasing rate from the precursor in this transformation.

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