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Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 36620-11-8, is researched, SMILESS is [F-][B+3]([F-])([F-])[F-].C12=C3[Rh+]14567(C8=C5C9C6=C7C8C9)C%10=C4C2CC3%10, Molecular C14H8BF4RhJournal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer, Author is Quiroz, Ryan V.; Reutershan, Michael H.; Schneider, Sebastian E.; Sloman, David; Lacey, Brian M.; Swalm, Brooke M.; Yeung, Charles S.; Gibeau, Craig; Spellman, Daniel S.; Rankic, Danica A.; Chen, Dapeng; Witter, David; Linn, Doug; Munsell, Erik; Feng, Guo; Xu, Haiyan; Hughes, Jonathan M. E.; Lim, Jongwon; Sauri, Josep; Geddes, Kristin; Wan, Murray; Mansueto, My Sam; Follmer, Nicole E.; Fier, Patrick S.; Siliphaivanh, Phieng; Daublain, Pierre; Palte, Rachel L.; Hayes, Robert P.; Lee, Sandra; Kawamura, Shuhei; Silverman, Steven; Sanyal, Sulagna; Henderson, Timothy J.; Ye, Yingchun; Gao, Yuanwei; Nicholson, Benjamin; Machacek, Michelle R., the main research direction is structure activity enzyme inhibiting; protein arginine methyltransferase catalyze dimethylation protein; mol docking human PRMT5 antitumor DNA repair methyltransferase.COA of Formula: C14H8BF4Rh.

Protein arginine methyltransferase 5 (PRMT5) is a type II arginine methyltransferase that catalyzes the post-translational sym. dimethylation of protein substrates. PRMT5 plays a critical role in regulating biol. processes including transcription, cell cycle progression, RNA splicing, and DNA repair. As such, dysregulation of PRMT5 activity is implicated in the development and progression of multiple cancers and is a target of growing clin. interest. Described herein are the structure-based drug designs, robust synthetic efforts, and lead optimization strategies toward the identification of two novel 5,5-fused bicyclic nucleoside-derived classes of potent and efficacious PRMT5 inhibitors. Utilization of compound docking and strain energy calculations inspired novel designs, and the development of flexible synthetic approaches enabled access to complex chemotypes with five contiguous stereo-centers. Addnl. efforts in balancing bioavailability, solubility, potency, and CYP3A4 inhibition led to the identification of diverse lead compounds with favorable profiles, promising in vivo activity, and low human dose projections.

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Quality Control of Bis(norbornadiene)rhodium (I) tetrafluoroborate. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: Bis(norbornadiene)rhodium (I) tetrafluoroborate, is researched, Molecular C14H8BF4Rh, CAS is 36620-11-8, about Azine-N-oxides as effective controlling groups for Rh-catalyzed intermolecular alkyne hydroacylation. Author is Moseley, Daniel F.; Kalepu, Jagadeesh; Willis, Michael C..

Azine N-oxide substituted aldehydes are used as highly effective substrates with good reactivity for intermol. hydroacylation of alkynes. Employing a Rh(I)-catalyst, a mild and scalable aldehyde C-H activation, that permits the coupling with unactivated terminal alkynes was achieved in good yields and with high regioselectivities (up to >20 : 1 l:b). Both substrates can tolerate a broad variety of functional groups. The reaction can also be applied to diazine aldehydes that contain a free N-lone pair. Conversion of the hydroacylation products to the corresponding azine, through a one-pot hydroacylation/deoxygenation sequence was also demonstrated. A one-pot hydroacylation/cyclization, using N-Boc propargylamine, addnl. leads to the synthesis of a bidentate pyrrolyl ligand.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Bis(norbornadiene)rhodium (I) tetrafluoroborate( cas:36620-11-8 ) is researched.Product Details of 36620-11-8.Cai, Nengjian; Mi, Fen; Wu, Yanmei; Song, Hao; Liu, Xiao-Yu; Qin, Yong published the article 《Practical and efficient preparation of the chiral 4-bromotryptophan derivative by Rh-catalyzed hydrogenation》 about this compound( cas:36620-11-8 ) in Tetrahedron Letters. Keywords: bromotryptophan enantioselective preparation rhodium catalyzed asym hydrogenation bromoindole. Let’s learn more about this compound (cas:36620-11-8).

An efficient three-step sequence has been developed for the preparation of a chiral 4-bromotryptophan derivative starting from the com. available 4-bromoindole. Key to the synthesis was the generation of the chiral center via a Rh-catalyzed asym. hydrogenation of a dehydrotryptophan precursor with 95% yield and >99% ee. Notably, the whole synthetic route required no column chromatog. operations and was readily conducted on large scales.

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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Bis(norbornadiene)rhodium (I) tetrafluoroborate, is researched, Molecular C14H8BF4Rh, CAS is 36620-11-8, about Highly Chemo- and Enantioselective Hydrogenation of 2-Substituted-4-oxo-2-alkenoic Acids.Safety of Bis(norbornadiene)rhodium (I) tetrafluoroborate.

The highly chemo- and enantioselective hydrogenation of (E)-2-substituted-4-oxo-2-alkenoic acids was established for the first time using the Rh/JosiPhos complex, affording a series of chiral α-substituted-γ-keto acids with excellent results (up to 99% yield and >99% ee) and high efficiency (up to 3000 TON). In addition, the importance of this methodol. was further demonstrated by a concise and gram-scale synthesis of the anti-inflammatory drug (R)-flobufen.

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Category: quinuclidine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: Bis(norbornadiene)rhodium (I) tetrafluoroborate, is researched, Molecular C14H8BF4Rh, CAS is 36620-11-8, about Highly chemo- and enantioselective Rh-catalyzed hydrogenation of β-sulfonyl-α,β-unsaturated ketones: Access to chiral γ-ketosulfones.

Rh-catalyzed highly chemo- and enantioselective hydrogenation of β-sulfonyl-α,β-unsaturated ketones was first successfully developed. Remarkably, a variety of enantioenriched γ-ketosulfones were generated in good to high yields with excellent chemo/enantioselectivities (82-99% yields, >99:1 chemoselectivity, 88 to >99% ee). Moreover, the gram-scale asym. hydrogenation was carried out smoothly in 97% yield and 97% ee. Preliminary DFT computations furnished a reasonable explanation for the high chemoselectivity and enantioselectivity.

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A series of RhI complexes featuring cationic diphosphinometal ligands (PMPn+) has been synthesized, and the effect of the dative RhI → Mn+ interactions on other ligands coordinated to the RhI center were studied. The Rh-CO bond strength in square pyramidal [(PMP)Rh(CO)X]n+-type complexes (X = Cl, H) is dominated by the charge of the metalloligand. Complex [(PZnP)Rh(CO)H](NTf2)2 (7) was evaluated for its competence in hydroformylation catalysis. Computational anal. of octahedral [(PMP)Rh(CO)2H]n+ model complexes revealed a strengthening of the Rh-CO bond trans to the metalloligand with increasing at. number of the metalloligand.

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Electric Literature of C14H8BF4Rh. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: Bis(norbornadiene)rhodium (I) tetrafluoroborate, is researched, Molecular C14H8BF4Rh, CAS is 36620-11-8, about Halogen bonding effects on the outcome of reactions at metal centres. Author is Carreras, Lucas; Benet-Buchholz, Jordi; Franconetti, Antonio; Frontera, Antonio; van Leeuwen, Piet W. N. M.; Vidal-Ferran, Anton.

Key findings regarding the effects of ligand preorganization via halogen bonding on the outcome of reactions at rhodium are reported. An unprecedented halogen bonding-mediated oxidative addition of CAr-I bonds to rhodium with efficient formation of cyclometalated species deserves special mention.

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A straightforward method to prepare 1,5-benzothiazepines was reported. Catalyzed by a Rh/Zhaophos complex, unsaturated cyclic NH lactams with a medium-size ring were hydrogenated smoothly, giving remarkably high enantioselectivities. The sulfur atom in the substrates did not bring an inhibition which was observed with com. available bisphosphine ligands. This method was successfully applied in the scale-up synthesis of (R)-(-)-thiazesim.

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13C-hyperpolarized carboxylates, such as pyruvate and acetate, are emerging mol. contrast agents for magnetic resonance imaging (MRI) visualization of various diseases, including cancer. Here, we present a systematic study of 1H and 13C parahydrogen-induced polarization of acetate and pyruvate esters with Et, Pr, and allyl alc. moieties. It was found that allyl pyruvate is the most efficiently hyperpolarized compound from those under study, yielding 21 and 5.4% polarization of 1H and 13C nuclei, resp., in CD3OD solutions Allyl pyruvate and Et acetate were also hyperpolarized in the aqueous phase using homogeneous hydrogenation with parahydrogen over a water-soluble rhodium catalyst. 13C polarization values of 0.82 and 2.1% were obtained for allyl pyruvate and Et acetate, resp. 13C-hyperpolarized methanolic and aqueous solutions of allyl pyruvate and Et acetate were employed for in vitro MRI visualization, demonstrating the prospects for translation of the presented approach to biomedical in vivo studies.

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Rh/ZhaoPhos-catalyzed asym. hydrogenation of a series of (E)-2-(chroman-4-ylidene)acetates I (R = H, Cl, F, MeO; R1 = CO2Me, CO2Et, CO2iPr) was successfully developed to prepare various chiral 4-substituted chromanes II with high yields and excellent enantioselectivities (up to 99% yield, 98% ee). Moreover, the gram-scale hydrogenation could be performed well in the presence of 0.02 mol% catalyst loading (TON = 5000) and the hydrogenation product II (R = H, R1 = CO2Et) was easily converted to access other important compounds, II (R = H, R1 = CO2H, CH2OH) which demonstrated the synthetic utility of this asym. catalytic methodol.

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