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Carboxy amido/carbene ligated Pd-complex catalyzed Suzuki-Miyaura cross-coupling of aryl-boronic acids with heteroaryl bromides is described. The protocol has a broad substrate scope that includes electron-rich, electron-deficient and sterically hindered arylboronic acids and heteroaryl bromides. The catalytic activity of the catalyst has been further investigated in the coupling of 2,6-dibromopyridine with arylboronic acids.

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Fosu, Hambira, and colleagues describe the direct C?H functionalization of medicinally relevant arenes or heteroarenes. This strategy is enabled by transient generation of reactive, non-symmetric iodanes from anions and PhI(OAc)2. The site-selective incorporation of Cl, Br, OMs, OTs, and OTf to complex molecules, including within medicines and natural products, can be conducted by the operationally simple procedure included herein. A computational model for predicting site selectivity is also included. The discovery of new medicines is a time- and labor-intensive process that frequently requires over a decade to complete. A major bottleneck is the synthesis of drug candidates, wherein each complex molecule must be prepared individually via a multi-step synthesis, frequently requiring a week of effort per molecule for thousands of candidates. As an alternate strategy, direct, post-synthetic functionalization of a lead candidate could enable this diversification in a single operation. In this article, we describe a new method for direct manipulation of drug-like molecules by incorporation of motifs with either known pharmaceutical value (halides) or that permit subsequent conversion (pseudo-halides) to medicinally relevant analogs. This user-friendly strategy is enabled by combining commercial iodine reagents with salts and acids. We expect this simple method for selective, post-synthetic incorporation of molecular diversity will streamline the discovery of new medicines. A strategy for C?H functionalization of arenes and heteroarenes has been developed to allow site-selective incorporation of various anions, including Cl, Br, OMs, OTs, and OTf. This approach is enabled by in situ generation of reactive, non-symmetric iodanes by combining anions and bench-stable PhI(OAc)2. The utility of this mechanism is demonstrated via para-selective chlorination of medicinally relevant arenes, as well as site-selective C?H chlorination of heteroarenes. Spectroscopic, computational, and competition experiments describe the unique nature, reactivity, and selectivity of these transient, unsymmetrical iodanes.

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Condensation of 2-carbamoylmethyl-1-methyl-3,4-dihydroisoquinolinium chloride with nicotinaldehyde in the presence of a catalytic amount of piperidine affords trans-3-carbamoyl-2-(3-pyridyl)-1,2,5,6-tetrahydro-3H- pyrrolo[2,1-a]isoquinolinium chloride.

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1,2-Dihydrocyclobutisoquinoline was synthesized through photochemical 2+2 cycloaddition of 3-methoxyisoquinolin-1(2H)-one to 1,1-dichloroethylene.Keywords – 1,2-dihydrocyclobutisoquinoline; photochemical 2+2 cycloaddition; photochemical synthesis; 1,2-dihydrocyclobutisoquinoline 4-substituted; zinc reduction; 1,1-dichloroethylene

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A novel hydrogen migration from the phenyl ring to the pyridine ring of an yttrium pyridyl complex supported by a 1,1?-ferrocene diamide ligand is reported. Density functional theory calculations were instrumental in probing the mechanism for this transformation.

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A number of quinolines and isoquinolines connected in various ways to a substituted benzimidazol-2-yl system were synthesized and evaluated as novel antagonists of adenosine receptors (ARs) by competition experiments using human A1, A2A, and A3 ARs. The new compounds were designed based on derivatives of 2-(benzimidazol-2-yl)quinoxaline, previously reported as potent and selective antagonists of A1 and A3 ARs. Among these, 3-[4-(ethylthio)-1H-benzimidazol-2-yl]isoquinoline 4b exhibited the best combination of potency toward the A1 AR (Ki=1.4nM) and selectivity against the A2A (Ki>10mum), A2B (Ki>10mum), and A3 ARs (Ki>1muM). Functional experiments in circular smooth muscle preparations of isolated human colon showed that 4b behaves as a potent and selective antagonist of the A1 AR in the neuromuscular compartment of this intestinal region. Biological and pharmacological data suggest that 4b is a suitable starting point for the development of novel agents endowed with stimulant properties on colonic activity.

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(Chemical Equation Presented) Propargylic diisopropylamines containing heterocycles, which were prepared readily from heterocyclic bromides and propargyldiisopropylamine by the Sonogashira coupling reaction, underwent the allene transformation reaction in the presence of Pd2(dba) 3·CHCl3 catalyst (2.5 mol %) and 1,2-bis[bis(pentafluorophenyl)phosphino]ethane (10 mol %) at 100C in CHCl3, giving the corresponding heterocyclic allenes in good to high yields via the palladium-catalyzed hydride-transfer reaction.

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We herein describe a chiral diboron-templated highly diastereoselective and enantioselective reductive coupling of isoquinolines that provided expedited access to a series of chiral substituted bisisoquinolines in good yields and excellent ee’s under mild conditions. The method enjoys a broad substrate scope and good functional group compatibility. Mechanistic investigation suggests the reaction proceeds through a concerted [3,3]-sigmatropic rearrangement.

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The invention discloses a benzo [b] thiophene compound and its application of obesity and in diabetes, Wherein: R1 , R2 , R3 , R4 Independently selected from the group of H, or CH F3 . Through the pharmacological activity experiment confirmed that the compound of the present invention 10 mum when the GOAT has better inhibition activity, can be used as inhibitors of GOAT obesity and diabetes disease in the animal model of more extensive pharmacological potency test, in order to receive the obesity and new medicine for treating diabetes. (by machine translation)

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An allyl group was attached to 3-keto function of ketolides in the presence of allyl bromide and KOtBu. Consequently, the Heck reaction of the resulting 2, 3-dehydro-3-O-allyl-10, 11-anhydroclarithromycin derivatives, in the presence of palladium (II) acetate and tri(o-tolyl)phosphine, afforded a 3-O-(3-aryl-E-prop-2-enyl) sidechain, not the previously reported 3-O-(3-aryl-Z-prop-1-enyl) sidechain. The results suggested that some steric factors in Beta-hydrogen elimination might regulate the isomerization. The activity of 2, 3-dehydro-3-O-(3-aryl-E-prop-2-enyl)-10, 11-anhydroclarithromycin derivatives was low.

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Isoquinoline – Wikipedia,
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