Tag: M.W=150-200

Furukawa, Naomichi published the artcileSelective ipso-substitution in pyridine ring and its application for the synthesis of macrocycles containing both oxa and thia bridges, Formula: C7H8ClNO, the main research area is macrocycle oxa thio bridge; pyridine sulfinyl sulfonyl ipso substitution; sulfonylpyridine ipso substitution; sulfonylpyridine.

Both the sulfinyl and sulfonyl groups directly bound to 2 or 4 position in pyridine were readily displaced by several nucleophiles such as RO- and RS- (R = alkyl, benzyl). The facility of the leaving groups is RSO2 �RSO > Br �Cl �RS. The ipso-substitution could be applied for the synthesis of new type of 2,6-disubstituted macrocycles I (n = 1, 2, 3) in moderate yields.

Tetrahedron Letters published new progress about macrocycle oxa thio bridge; pyridine sulfinyl sulfonyl ipso substitution; sulfonylpyridine ipso substitution; sulfonylpyridine. 42144-78-5 belongs to class pyridine-derivatives, name is 2-Chloro-6-ethoxypyridine, and the molecular formula is C7H8ClNO, Formula: C7H8ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kametani, Tetsuji published the artcileSyntheses of heterocyclic compounds. CCCLXXI. Synthetic approach to camptothecin, SDS of cas: 21190-89-6, the main research area is camptothecin analog; indolizinoquinoline; quinoline indolizino; pyrrolidinopyridone; pyridone pyrrolidino.

Picolinic acid 1-oxide was esterified with SOCl2 and EtOH to the Et ester, whose treatment with phosphoryl chloride gave Et 6-chloropicolinate (I). Hydrolysis of I with HCl gave 6-oxo-1,6-dihydropicolinic acid (II). Simultaneous condensation and cyclization of the Me ester of II with Me acrylate in the presence of sodium carbonate in DMF yielded the Me, 1,2,3,5-tetrahydro-1,5-dioxoindolizine-2-carboxylate (III). Hydrolysis and decarboxylation of III with HCl gave 3-oxo-pyrrolidino[2,1-f]-2-pyridone (IV). Friedlaender condensation of IV with 2-aminobenzaldehyde gave a camptothecin analog, 9,11-dihydro-9-oxoindolizino[1,2-b]quinoline (V).

Tetrahedron published new progress about camptothecin analog; indolizinoquinoline; quinoline indolizino; pyrrolidinopyridone; pyridone pyrrolidino. 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, SDS of cas: 21190-89-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

De Roos, K. B. published the artcileDeazapurine derivatives. V. New synthesis of 1- and 3-deaza-adenine and related compounds, Product Details of C7H6ClNO2, the main research area is adenines deaza; deazaadenines; imidazopyridines; pyridines imidazo; purines deaza.

Reinvestigation of the cyclization of 2,3,4-triaminopyridine by several procedures showed that both 7-aminoimidazo[4,5-b]pyridine (1-deaza-adenine) (I) and 4-aminoimidazo[4,5-c]pyridine (3-deazaadenine) (II) were always obtained. A new and convenient route to the synthesis of I was devised. An unambiguous synthesis of II is given. Ring closure of 2,4,5-triaminopyridine afforded 6-aminoimidazo[4,5-c]pyridine (3-deazaisoadenine).

Recueil des Travaux Chimiques des Pays-Bas published new progress about adenines deaza; deazaadenines; imidazopyridines; pyridines imidazo; purines deaza. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Product Details of C7H6ClNO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Gudmundsson, Kristjan S. published the artcileAn improved large-scale synthesis of 2-amino-4-chloropyridine and its use for the convenient preparation of various polychlorinated 2-aminopyridines, Recommanded Product: Methyl 4-chloropicolinate, the main research area is aminochloropyridine preparation chlorination; polychlorinated aminopyridine preparation; pyridine amino polychlorinated preparation.

An efficient large scale synthesis of 2-amino-4-chloropyridine (I) has been achieved through a modification of existing literature procedures. I was used to prepare the previously unreported 2-amino-4,5-dichloropyridine. The known 2-amino-3,4-dichloropyridine and 2-amino-3,4,5-trichloropyridine were prepared from I by new routes and in higher yields than previously reported.

Synthetic Communications published new progress about aminochloropyridine preparation chlorination; polychlorinated aminopyridine preparation; pyridine amino polychlorinated preparation. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Recommanded Product: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Asakawa, Chiharu published the artcile[11C]Sorafenib: Radiosynthesis and preliminary PET study of brain uptake in P-gp/Bcrp knockout mice, Application of Methyl 4-chloropicolinate, the main research area is carbon 11 sorafenib preparation PET imaging brain.

Sorafenib (Nexavar, BAY43-9006, 1) is a second-generation, orally active multikinase inhibitor that is approved for the treatment of some cancers in patients. In this Letter, we developed [11C]1 as a novel positron emission tomog. (PET) probe, and evaluated the influence of ABC transporters-mediated efflux on brain uptake using PET with [11C]1 in P-glycoprotein (P-gp)/breast cancer resistance protein (Bcrp) knockout mice vs. wild-type mice. [11C]1 was synthesized by the reaction of hydrochloride of aniline 2 with [11C]phosgene ([11C]COCl2) to give isocyanate [11C]6, followed by reaction with another aniline 3. Small-animal PET study with [11C]1 indicated that the radioactivity level (AUC0-60 min, SUV × min) in the brains of P-gp/Bcrp knockout mice was about three times higher than in wild-type mice.

Bioorganic & Medicinal Chemistry Letters published new progress about Brain. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Application of Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Bezencon, Olivier published the artcileDesign and Preparation of Potent, Nonpeptidic, Bioavailable Renin Inhibitors, Safety of 2-chloro-3-methylisonicotinaldehyde, the main research area is aryl substituted diazabicyclononenecarboxamide preparation selective renin inhibitor antihypertensive; potent nonpeptidic bioavailable diazabicyclononenecarboxamide renin inhibitor; structure aryl substituted diazabicyclononenecarboxamide inhibition renin; mol crystal structure renin bound nonracemic aryloxyethylphenyl diazabicyclononenecarboxamide.

Aryl-substituted diazabicyclononenecarboxamides such as I are prepared as selective human renin inhibitors for potential use as antihypertensive agents. Aryl substituents and the carboxamide moiety of the diazabicyclononenecarboxamides are essential for selective binding to renin; attachment of a substituent to the methyleneaminomethylene bridge of the diazabicyclononenecarboxamides does not modify the binding affinity but alters the pharmacokinetics of the product. I inhibits renin with an IC50 of 0.20 nM in buffer and 19 nM in plasma; a 10 mg/kg dose of I lowers the blood pressures of transgenic rats over a period of 36 h. The structures of both enantiomers of an aryloxyethylphenyl diazabicyclononenecarboxamide sep. bound to human renin are determined by X-ray crystallog.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 790696-96-7 belongs to class pyridine-derivatives, name is 2-chloro-3-methylisonicotinaldehyde, and the molecular formula is C7H6ClNO, Safety of 2-chloro-3-methylisonicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Chengwei published the artcileStudy on Typical Diarylurea Drugs or Derivatives in Cocrystallizing with Strong H-Bond Acceptor DMSO, Name: Methyl 4-chloropicolinate, the main research area is diarylurea drug derivative cocrystn DMSO.

Diarylureas are widely used in self-assembly and supramol. chem. owing to their outstanding characteristics as both H-bond donors and acceptors. Unfortunately, this bonding property is rarely applied in the development of urea-containing drugs. Herein, seven related DMSO complexes were screened from 12 substrates involving sorafenib and regorafenib, mainly considering the substitution effect following a robust procedure. All complexes were structurally confirmed by spectroscopic means and thermal anal. Specially, five cocrystals with three deuterated, named sorafenib·DMSO, donafenib·DMSO, deuregorafenib·DMSO, 6·DMSO, and 7·DMSO were obtained. The crystal structures revealed that all host mols. consistently bonded with DMSO in intermol. interaction in a 1:1 stoichiometry. However, further comparison with documented DMSO complexes and parent motifs presented some arrangement diversities especially for 6·DMSO which offered a counter-example to previous rules. Major changes in the orientation of meta-substituents and the packing stability for sorafenib·DMSO and deuregorafenib·DMSO were rationalized by theory anal. and computational energy calculation Cumulative data implied that the planarization of two aryl planes in diarylureas may play a crucial role in cocrystn. Also, a polymorph study bridged the transformation between these ureas and their DMSO complexes.

ACS Omega published new progress about Cocrystallization. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Name: Methyl 4-chloropicolinate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hansen, Helge-Boj published the artcileThe Stronger the Better: Donor Substituents Push Catalytic Activity of Molecular Chromium Olefin Polymerization Catalysts, Category: pyridine-derivatives, the main research area is donor substituents chromium; chromium, ligand effects, olefin polymerization, supported catalysts, UHMW-PE.

The donor strength of bifunctional pyridine-cyclopentadienyl ligands was altered systematically by the introduction of donating groups in the para-position of the pyridine. In the resulting chromium complexes an almost linear correlation between donor strength and the nitrogen-chromium distance as well as the electronic absorption maximum is exptl. observed The connection of electron-donating groups in the ligand backbone leads to an efficient transfer of the electronic influences to the catalytically active metal center without restricting it through steric effects. Therefore, catalytic olefin polymerization activity, which is already very high for the previously studied catalysts, increase considerably by attaching para-amino groups to the chelating pyridine or quinoline, resp. Combining electron-rich indenyl ligands with para-amino substituted pyridines lead to the highest catalytic activities observed so far for this class of organo chromium olefin polymerization catalysts. The resulting polymers are of ultra-high mol. weight and the ability of the catalysts to incorporate co-monomers is also very high.

Chemistry – A European Journal published new progress about Crystal structure. 24484-93-3 belongs to class pyridine-derivatives, name is Methyl 4-chloropicolinate, and the molecular formula is C7H6ClNO2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ogasawara, Daisuke published the artcileDiscovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12), Product Details of C6H5Cl2N, the main research area is lysophosphatidylserine lipase hydrolase domain 12 ABHD12 inhibitor.

ABHD12 is a membrane-bound hydrolytic enzyme that acts on the lysophosphatidylserine (lyso-PS) and lysophosphatidylinositol (lyso-PI) classes of immunomodulatory lipids. Human and mouse genetic studies point to a key role for the ABHD12-(lyso)-PS/PI pathway in regulating (neuro)immunol. functions in both the central nervous system and periphery. Selective inhibitors of ABHD12 would offer valuable pharmacol. probes to complement genetic models of ABHD12-regulated (lyso)-PS/PI metabolism and signaling. Here, we provide a detailed description of the discovery and activity-based protein profiling (ABPP) guided optimization of reversible thiourea inhibitors of ABHD12 that culminated in the identification of DO264 as a potent, selective, and in vivo active ABHD12 inhibitor. We also show that DO264, but not a structurally related inactive control probe (S)-DO271, augments inflammatory cytokine production from human THP-1 macrophage cells. The in vitro and in vivo properties of DO264 designate this compound as a suitable chem. probe for studying the biol. functions of ABHD12-(lyso)-PS/PI pathways.

Journal of Medicinal Chemistry published new progress about Crystal structure. 132097-09-7 belongs to class pyridine-derivatives, name is 2,4-Dichloro-3-methylpyridine, and the molecular formula is C6H5Cl2N, Product Details of C6H5Cl2N.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mandal, Mihirbaran published the artcileDesign and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme-1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation, Synthetic Route of 917471-30-8, the main research area is bicyclic iminopyrimidinone preparation BACE1 inhibitor amyloid Alzheimer’s.

On the basis of our observation that the biaryl substituent of iminopyrimidinone 7 must be in a pseudoaxial conformation to occupy the contiguous S1-S3 subsites of BACE1, we have designed a novel fused bicyclic iminopyrimidinone scaffold intended to favor this bioactive conformation. Strategic incorporation of a nitrogen atom in the new constrained ring allowed us to develop SAR around the S2′ binding pocket and ultimately resulted in analogs with low nanomolar potency for BACE1. In particular, optimization of the prime side substituent led to major improvements in potency by displacement of two conserved water mols. from a region near S2′. Further optimization of the pharmacokinetic properties of this fused pyrrolidine series, in conjunction with facile access to a rat pharmacodynamic model, led to identification of compound 43, which is an orally active, brain penetrant inhibitor that reduces Aβ40 in the plasma, CSF, and cortex of rats in a dose-dependent manner.

Journal of Medicinal Chemistry published new progress about Alzheimer disease. 917471-30-8 belongs to class pyridine-derivatives, name is (5-(Prop-1-yn-1-yl)pyridin-3-yl)boronic acid, and the molecular formula is C8H8BNO2, Synthetic Route of 917471-30-8.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem