Month: December 2022

Li, Hong-Liang published the artcilePalladium-Catalyzed Enantioselective C(sp³)-H Arylation of 2-Propyl Azaaryls Enabled by an Amino Acid Ligand, Product Details of C6H13I, the publication is Organic Letters (2022), 24(6), 1286-1291, database is CAplus and MEDLINE.

A palladium(II)-catalyzed enantioselective arylation of unbiased secondary C(sp3)-H bonds was developed. The enantioselectivity was controlled by the combination of a pyridyl or isoquinolinyl directing group and an amino acid, N-Boc-2-pentyl proline. A variety of 2-Pr azaaryls and biaryl iodides were employed to provide arylated products in moderate to good yields (up to 82%) with high enantioselectivities (up to 93:7 er). This reaction is a rare example of an amino-acid-enabled enantioselective acyclic methylene C(sp3)-H arylation. Furthermore, the reaction proceeded with high enantioselectivity even on a gram scale, and the product was transformed to a 5,6,7,8-tetrahydroisoquinoline bioactive mol. Kinetic isotope effect (KIE) experiments indicated that C-H activation is the rate-determining step for the enantioselective C(sp3)-H arylation.

Organic Letters published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C6H13I, Product Details of C6H13I.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Zhang, Zhen-Qi published the artcileCopper-Catalyzed/Promoted Cross-coupling of gem-Diborylalkanes with Nonactivated Primary Alkyl Halides: An Alternative Route to Alkylboronic Esters, Synthetic Route of 161370-66-7, the publication is Organic Letters (2014), 16(24), 6342-6345, database is CAplus and MEDLINE.

The first copper-catalyzed/promoted sp³-C Suzuki-Miyaura coupling reaction of gem-diborylalkanes with nonactivated electrophilic reagents is reported. Not only 1,1-diborylalkanes but also some other gem-diborylalkanes can be coupled with nonactivated primary alkyl halides, offering a new method for sp³C-sp³C bond formation and, simultaneously, providing a new strategy for the synthesis of alkylboronic esters.

Organic Letters published new progress about 161370-66-7. 161370-66-7 belongs to iodides-buliding-blocks, auxiliary class Chiral,Iodide,Amine,Aliphatic hydrocarbon chain,Ester,Amide, name is (S)-tert-Butyl 2-((tert-butoxycarbonyl)amino)-4-iodobutanoate, and the molecular formula is C6H8BNO3, Synthetic Route of 161370-66-7.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Tian, Chengze published the artcileDiscovery of cinnoline derivatives as potent PI3K inhibitors with antiproliferative activity, Quality Control of 638-45-9, the publication is Bioorganic & Medicinal Chemistry Letters (2021), 128271, database is CAplus and MEDLINE.

Cinnoline is a potential pharmacophore which has rarely been reported for uses as PI3K inhibitors. In this study, a series of cinnoline derivatives were developed as PI3K inhibitors and evaluated for enzymic and cellular activities. Most compounds displayed nanomolar inhibitory activities against PI3Ks, among which 25 displayed high LLE and micromolar inhibitory potency against three human tumor cell lines (IC₅₀ = 0.264μM, 2.04μM, 1.14μM).

Bioorganic & Medicinal Chemistry Letters published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C18H34N4O5S, Quality Control of 638-45-9.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Lazaro-Milla, Carlos published the artcileMetal-Free C-C/C-N/C-C Bond Formation Cascade for the Synthesis of (Trifluoromethyl)sulfonylated Cyclopenta[b]indolines, Formula: C7H8INO, the publication is Organic Letters (2021), 23(8), 2921-2926, database is CAplus and MEDLINE.

A bis(triflyl)ethylation [triflyl = (trifluoromethyl)sulfonyl] inserted into a sequential cyclization cascade resulted in the direct formation of gem-bis(triflyl)ated cyclopenta[b]indolines from anilide-derived allenols and alkenols. This catalyst- and irradiation-free sequence facilitated the efficient preparation of functionalized tricyclic indoline cores bearing two contiguous stereocenters. The formed cyclopenta[b]indolines was easily transformed into a wide variety of triflylated indolines, including the tetracycle ring system found in polyveoline.

Organic Letters published new progress about 53279-83-7. 53279-83-7 belongs to iodides-buliding-blocks, auxiliary class Iodide,Amine,Benzene,Alcohol, name is (2-Amino-5-iodophenyl)methanol, and the molecular formula is C7H8INO, Formula: C7H8INO.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Miles, Dillon H. published the artcileDiscovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3Kγ Inhibitors, Category: iodides-buliding-blocks, the publication is ACS Medicinal Chemistry Letters (2020), 11(11), 2244-2252, database is CAplus and MEDLINE.

The successful application of immunotherapy in the treatment of cancer relies on effective engagement of immune cells in the tumor microenvironment. Phosphoinositide 3-kinase γ (PI3Kγ) is highly expressed in tumor-associated macrophages, and its expression levels are associated with tumor immunosuppression and growth. Selective inhibition of PI3Kγ offers a promising strategy in immuno-oncol., which has led to the development of numerous potent PI3Kγ inhibitors with variable selectivity profiles. To facilitate further investigation of the therapeutic potential of PI3Kγ inhibition, we required a potent and PI3Kγ-selective tool compound with sufficient metabolic stability for use in future in vivo studies. Herein, we describe some of our efforts to realize this goal through the systematic study of SARs within a series of 7-azaindole-based PI3Kγ inhibitors. The large volume of data generated from this study helped guide our subsequent lead optimization efforts and will inform further development of PI3Kγ-selective inhibitors for use in immunomodulation.

ACS Medicinal Chemistry Letters published new progress about 757978-19-1. 757978-19-1 belongs to iodides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Bromide,Iodide,Sulfamide,Benzene, name is 5-Bromo-3-iodo-1-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine, and the molecular formula is C13H8BrIN2O2S, Category: iodides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Yuan, Chen published the artcileDiscovery of [1,2,4]triazole derivatives as new metallo-β-lactamase inhibitors, Quality Control of 39115-95-2, the publication is Molecules (2020), 25(1), 56, database is CAplus and MEDLINE.

The emergence and spread of metallo-β-lactamase (MBL)-mediated resistance to β-lactam antibacterials has already threatened the global public health. A clin. useful MBL inhibitor that can reverse β-lactam resistance has not been established yet. We here report a series of [1,2,4]triazole derivatives and analogs, which displayed inhibition to the clin. relevant subclass B1 (Verona integron-encoded MBL-2) VIM-2. 3-(4-Bromophenyl)-6,7-dihydro-5H-[1,2,4]triazolo [3,4-b][1,3]thiazine (5l) manifested the most potent inhibition with an IC50 (half-maximal inhibitory concentration) value of 38.36μM. Investigations of 5l against other B1 MBLs and the serine β-lactamases (SBLs) revealed the selectivity to VIM-2. Mol. docking analyses suggested that 5l bound to the VIM-2 active site via the triazole involving zinc coordination and made hydrophobic interactions with the residues Phe61 and Tyr67 on the flexible L1 loop. This work provided new triazole-based MBL inhibitors and may aid efforts to develop new types of inhibitors combating MBL-mediated resistance.

Molecules published new progress about 39115-95-2. 39115-95-2 belongs to iodides-buliding-blocks, auxiliary class Iodide,Hydrazine,Amine,Benzene,Hydrazide,Amide, name is 4-Iodobenzohydrazide, and the molecular formula is C9H7N5O, Quality Control of 39115-95-2.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Chen, Yuqing published the artcileSynthesis of Homoallylic Amines by Radical Allylation of Imines with Butadiene under Photoredox Catalysis, HPLC of Formula: 638-45-9, the publication is Angewandte Chemie, International Edition (2022), 61(29), e202204516, database is CAplus and MEDLINE.

A conceptually different radical-radical cross-coupling strategy for the synthesis of a homoallyl amines RCH₂CH=CHCH₂CH(NHR¹)(R²) (R = oxetan-3-yl, 3-methylbut-3-en-1-yl, 2-(tert-butoxy)-2-oxoethyl, etc.; R¹ = 4-fluorophenyl, 2,4,6-trimethylphenyl, naphthalen-2-yl, etc.; R² = thiophen-2-yl, 3,4-dimethoxyphenyl, 4-[methoxy(oxo)methyl]phenyl, etc.) between an α-amino alkyl radical and a transient allylic radical have been reported. This metal-free method provided a novel approach for the synthesis of homoallylic amines (>80 examples) from readily available materials with excellent regioselectivity and exceptional broad functional group compatibility.

Angewandte Chemie, International Edition published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C6H13I, HPLC of Formula: 638-45-9.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Hattori, Yoshihide published the artcileSynthesis and evaluation as MRI probe of the trifluoromethylated p-boronophenylalanine and its alcohol derivative, Computed Properties of 364-12-5, the publication is Bioorganic & Medicinal Chemistry (2007), 15(5), 2198-2205, database is CAplus and MEDLINE.

Boron-neutron capture therapy (BNCT) and magnetic resonance imaging (MRI) are quite attractive techniques for treatment and diagnosis of cancer, resp. In order to develop practical tools for BNCT and MRI, novel compounds containing both the trifluoromethyl group and ¹⁰B atom in a single mol. were designed. In the present study, p-boronophenylalanine and p-boronophenylalaninol with the trifluoromethyl group were synthesized, and ¹⁹F NMR measurements of these compounds were carried out.

Bioorganic & Medicinal Chemistry published new progress about 364-12-5. 364-12-5 belongs to iodides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,Iodide,Benzene, name is 5-Bromo-2-iodobenzotrifluoride, and the molecular formula is C7H3BrF3I, Computed Properties of 364-12-5.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Shinohara, Mai published the artcilePhoto-control of Cellular Uptake by the Selective Adsorption of Spiropyran Derivatives on Albumin, HPLC of Formula: 638-45-9, the publication is Chemistry Letters (2022), 51(6), 594-597, database is CAplus.

A photochromic spiropyran derivative (SP6) as a drug tag was prepared SP6 was selectively taken up into cells by photo-controlling the adsorption on albumin, which has attracted attention as a carrier for delivering drugs to tumor cells. The desorption of SP6 from albumin was achieved via the isomerization and hydrolysis of SP6.

Chemistry Letters published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C3H6BrNaO3S, HPLC of Formula: 638-45-9.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Kuai, Chang-Sheng published the artcilePalladium-Catalyzed Regio- and Stereoselective Hydroaminocarbonylation of Unsymmetrical Internal Alkynes toward α,β-Unsaturated Amides, COA of Formula: C6H13I, the publication is Organic Letters (2022), 24(24), 4464-4469, database is CAplus and MEDLINE.

α,β-Unsaturated amides play a vital role in natural products, pharmaceuticals, organic synthesis, and functional materials. Herein, authors disclosed a regio- and stereoselective hydroaminocarbonylation of unsym. internal alkynes via palladium catalysis to synthesize α,β-unsaturated amides. This protocol features excellent regio- and exclusive (E)-stereoselectivity, high atom and step-economy, broad substrate scope, and functional group tolerance.

Organic Letters published new progress about 638-45-9. 638-45-9 belongs to iodides-buliding-blocks, auxiliary class Iodide,Aliphatic hydrocarbon chain, name is 1-Iodohexane, and the molecular formula is C6H13I, COA of Formula: C6H13I.

Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com