Tag: M.W=250-300

Weiss, Matthew M. published the artcileSulfonamides as Selective Na_V1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities, Name: 6-Bromo-1,4-dichlorophthalazine, the publication is Journal of Medicinal Chemistry (2017), 60(14), 5969-5989, database is CAplus and MEDLINE.

Several reports have recently emerged regarding the identification of heteroarylsulfonamides as Na_V1.7 inhibitors that demonstrate high levels of selectivity over other Na_V isoforms. The optimization of a series of internal Na_V1.7 leads that address a number of metabolic liabilities including bioactivation, PXR activation, as well as CYP3A4 induction and inhibition led to the identification of potent and selective inhibitors that demonstrated favorable pharmacokinetic profiles and were devoid of the aforementioned liabilities. The key to achieving this within a series prone to transporter-mediated clearance was the identification of a small range of optimal cLogD values and the discovery of subtle PXR SAR that was not lipophilicity dependent. This enabled the identification of compound 20, which was advanced into a target engagement pharmacodynamic model where it exhibited robust reversal of histamine-induced scratching bouts in mice.

Journal of Medicinal Chemistry published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H11NO, Name: 6-Bromo-1,4-dichlorophthalazine.

Im, Jeong Kyun published the artcileN-Chlorinative Ring Contraction of 1,4-Dimethoxyphthalazines via a Bicyclization/Ring-Opening Mechanism, Application of 6-Bromo-1,4-dichlorophthalazine, the publication is Synthesis (2021), 53(10), 1760-1770, database is CAplus.

An unprecedented N-chlorinative ring contraction of 1,2-diazines was discovered and investigated with an electrophilic chlorinating reagent, trichloroisocyanuric acid (TCICA). Through optimization and mechanistic anal., the assisting role of n-Bu4NCl as an exogenous nucleophile was identified and the optimized reaction conditions were applied to a range of 1,4-dimethoxyphthalazine derivatives Also, an improvement of overall efficiency was demonstrated by the use of a labile O-silyl group. A bicyclization/ring-opening mechanism inspired by the Favorskii rearrangement was proposed and supported by the DFT calculations Furthermore, the efforts on scope expansion as well as the evaluation of other electrophilic promoters revealed that the newly developed ring contraction reactivity was a unique characteristic of 1,4-dimethoxyphthalazine scaffold and TCICA.

Synthesis published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H3BrCl2N2, Application of 6-Bromo-1,4-dichlorophthalazine.

Kuroboshi, Manabu published the artcileAsymmetric dihydroxylation of olefins in a chiral ligand-immobilized silica-gel/water disperse system, COA of Formula: C8H3BrCl2N2, the publication is Proceedings – Electrochemical Society (2003), 141-144, database is CAplus.

A newly designed (DHQD)₂PHAL-type ligand was synthesized and immobilized on silica gel at the phtharadine unit. Asym. dihydroxylation of olefins was carried out in a disperse system with (DHQD)₂PHAL-immobilized silica gel as a disperse phase and an aqueous NaHCO₃-K₃Fe(CN)₆ as a disperse media to give the corresponding diols in moderate to good yields and enantiomeric excess. Recycle use of the (DHQD)₂PHAL-immobilized silica gel was successfully achieved.

Proceedings – Electrochemical Society published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H3BrCl2N2, COA of Formula: C8H3BrCl2N2.

Im, Jeong Kyun published the artcileN-Chlorination-induced, oxidative ring contraction of 1,4-dimethoxyphthalazines, SDS of cas: 240400-95-7, the publication is Tetrahedron Letters (2020), 61(26), 152048, database is CAplus.

A rarely explored oxidative ring contraction of electron-rich 1,2-diazine was described. Upon treatment with an electrophilic chlorinating reagent (TCICA), 1,4-dimethoxyphthalazines undergo an N-chlorination-induced ring contraction that was accompanied by the loss of one nitrogen atom. The scope of this unusual reactivity was examined with a range of 1,4-dimethoxyphthalazine derivatives In addition, a mechanism proceeding via a bicyclic species was proposed on the basis of an isolated reaction intermediate and DFT calculations

Tetrahedron Letters published new progress about 240400-95-7. 240400-95-7 belongs to phthalazine, auxiliary class Chloride,Bromide,Phthalazine, name is 6-Bromo-1,4-dichlorophthalazine, and the molecular formula is C8H3BrCl2N2, SDS of cas: 240400-95-7.