Flexible application of 7-Bromophthalazin-1(2H)-one in synthetic route

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Rate laws may be derived directly from the chemical equations for elementary reactions. This is not the case, however, for ordinary chemical reactions.7-Bromophthalazin-1(2H)-one, cas is 152265-57-1,the phthalazine compound, below Introduce a new synthetic route., 152265-57-1

10198] 7-l3romo- 1 -chlorophthalazine (9a) In a flame dried25 mE round bottom flask was added 7-bromophthalazin-1 (2H)-one (205 mg, 0.91 mmol), anhydrous acetonitrile (9 mE), and phosphorus oxychloride (0.3 mE, 3.22 mmol). The mixture was refluxed for 2 hours, then cooled to 00 C., diluted with dichloromethane (20 mE), and quenched with a drop- wise addition of sat. aq. NaHCO3 (20 mE). The biphasic mixture was stirred vigorously and allowed to warm to room temperature. Afier 1 hour the layers were separated and the aqueous was extractedwith dichioromethane (2×30 mE). The combined organic layers were washed with sat. aq. NaHCO3 (25 mE), washed with brine (20 mE), dried over Na2SO4, and concentrated to yield 9a as an orange solid in 91% yield. ?HNMR (500 MHz, CDC13) oe 9.45 (s, 1H), 8.49-8.5 1 (m, 1H), 8.10 (dd, J=8.8, 2.0 Hz, 1H), 7.91 (d, J=8.8 Hz, 1H). ECMS found 242.9 [M+H].

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Reference£º
Patent; Northeastern University; POLLASTRI, Michael P.; MEHTA, Naimee; DEVINE, William; WOODRING, Jennifer; SWAMINATHAN, Uma; US2015/259331; (2015); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

The effect of 152265-57-1 reaction temperature change on equilibrium

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A heterogeneous catalyst is a catalyst that is present in a different phase than the reactants. Such catalysts generally function by furnishing an active surface upon which a reaction can occur. 152265-57-1, name is 7-Bromophthalazin-1(2H)-one, introduce a new downstream synthesis route as follows. 152265-57-1

Bis(pinacolato)diboron (1.1 equiv), potassium acetate (3.5 equiv) and 1,1′- bis(diphenylphosphino)ferrocene (0.05 equiv) were dissolved in dioxane. The mixture was degassed with nitrogen for 20 minutes before the addition of PdCl2(dppf) (0.05 equiv). The mixture was degassed for a further 5 minutes. The mixture was heated to reflux for 16 hours and then allowed to cool to room temperature. Water was added to the mixture before it was extracted with EtOAc (2 X 2 reaction volumes). The combined organic fractions were dried (MgSO4), filtered aned concentrated in vacuo before being purified by flash chromatography (SiO2) neat hexanes going to 1 : 1 – Hexanes:EtOAc then neat EtOAc to give the desire product as a white crystalline solid.7-(4,4,5,5-Tetramethyl-[l,3,2]dioxaborolan-2-yl)-2H-phthalazin-l-one: (86 % yield, 92 % purity) m/z (LC-MS5ESP): 191.3 [M+H]+, R/T = 2.29 min)

Other significant industrial processes that involve the use of heterogeneous catalysts include the preparation of sulfuric acid, the preparation of ammonia, the oxidation of ammonia to nitric acid, and the synthesis of methanol.152265-57-1, if you are interested, you can browse my other articles.

Reference£º
Patent; KUDOS PHARMACEUTICALS LIMITED; WO2008/23161; (2008); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

Little discovery in the laboratory: a new route for 152265-57-1

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We know that the rate of many reactions can be accelerated by catalysts. A catalyst speeds up the rate of a reaction by lowering the activation energy; in addition, the catalyst is regenerated in the process. 7-Bromophthalazin-1(2H)-one, cas is 152265-57-1,the phthalazine compound, below Introduce a new synthetic route., 152265-57-1

A mixture of compound 50-d (600mg, 2.67mmol) and POCl3 (8mL) was heated to reflux for 1.5h, cooled toroom temperature and concentrated under reduced pressure. The residue was dissolved in DCM (40mL), washed inturn with saturated sodium bicarbonate (40mL) and saturated brine (10mL), dried over anhydrous sodium sulfate, filteredand concentrated under reduced pressure. The residue was purified by silica column chromatography (PE:EA = 3:1) togive compound 50-c (500mg, yield 75%). LC-MS (ESI): m/z = 243 [M+H]+.

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Reference£º
Patent; Shanghai Yingli Pharmaceutical Co. Ltd.; XU, Zusheng; ZHANG, Nong; SUN, Qingrui; WU, Tianzhi; (104 pag.)EP3275867; (2018); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

The effect of 152265-57-1 reaction temperature change on equilibrium

Other significant industrial processes that involve the use of heterogeneous catalysts include the preparation of sulfuric acid, the preparation of ammonia, the oxidation of ammonia to nitric acid, and the synthesis of methanol.152265-57-1, if you are interested, you can browse my other articles.

A heterogeneous catalyst is a catalyst that is present in a different phase than the reactants. Such catalysts generally function by furnishing an active surface upon which a reaction can occur. 152265-57-1, name is 7-Bromophthalazin-1(2H)-one, introduce a new downstream synthesis route as follows. 152265-57-1

To a stirred solution of 7-bromophthalazin-l(2H)-one (1,00 g, 4.44 mmol, 1,0 eq) in DMF (10 ml) was added 2-(chloromethyl)- oxirane (1.24 g, 13 3 mmol, 3.0 eq) and CS2CO3 (4.35 g, 13.3 mmol, 3.0 eq), and the resultant mixture was heated to 90 C for 0.5 hour. The reaction mixture was diluted with cold water, and was extracted with EA. Organic phase was washed with water twice followed by brine, dried over MgS04, and was concentrated to dryness. The obtained residue was used directly in next step without further purification.

Other significant industrial processes that involve the use of heterogeneous catalysts include the preparation of sulfuric acid, the preparation of ammonia, the oxidation of ammonia to nitric acid, and the synthesis of methanol.152265-57-1, if you are interested, you can browse my other articles.

Reference£º
Patent; PHARMABLOCK SCIENCES (NANJING), INC.; LIU, Liu; LI, Jin; YANG, Minmin; (126 pag.)WO2019/173804; (2019); A1;,
Phthalazine – Wikipedia
Phthalazine | C8H6N2 – PubChem

Extended knowledge of 152265-57-1

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Rhodium(III)-Catalyzed C-H Functionalization of 1-(2H)-Phthalazinones at C8

The rhodium(III) catalyst tris(acetonitrile)pentamethylcyclopentadienylrhodium(III) hexafluoroantimonate ([Cp*Rh(MeCN)3](SbF6)2) reacts with 1-(2H)-phthalazinones to promote a C-H functionalization event at C8. Preparation of a set of compounds arising from oxidative alkenylation with olefins, hydroarylation with alkynes, and iodination with N-iodosuccinimide is reported here. Oxidative alkenylation proceeds in very good yield, and the scope and limitations of the hydroarylation and halogenation reactions are discussed. Notably, this strategy enables rapid preparation of C8-substituted phthalazinones without requiring phthalazinone ring synthesis starting from a prefunctionalized arene.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N712 – PubChem

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2-METHYLMORPHOLINE PYRIDO-, PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS

There is provided a compound of Formula (I), or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula (1), and the use of a compound of Formula (1) as a medicament and in the treatment of cancer

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Phthalazine – Wikipedia,
Phthalazine | C8H6N706 – PubChem

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Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery

Tropical protozoal infections are a significant cause of morbidity and mortality worldwide; four in particular (human African trypanosomiasis (HAT), Chagas disease, cutaneous leishmaniasis, and malaria) have an estimated combined burden of over 87 million disability-adjusted life years. New drugs are needed for each of these diseases. Building on the previous identification of NEU-617 (1) as a potent and nontoxic inhibitor of proliferation for the HAT pathogen (Trypanosoma brucei), we have now tested this class of analogs against other protozoal species: T. cruzi (Chagas disease), Leishmania major (cutaneous leishmaniasis), and Plasmodium falciparum (malaria). Based on hits identified in this screening campaign, we describe the preparation of several replacements for the quinazoline scaffold and report these inhibitors’ biological activities against these parasites. In doing this, we have identified several potent proliferation inhibitors for each pathogen, such as 4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)-6-(4-((4-methyl-1,4-diazepan-1-yl)sulfonyl)phenyl)quinoline-3-carbonitrile (NEU-924, 83) for T. cruzi and N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-7-(4-((4-methyl-1,4-diazepan-1-yl)sulfonyl)phenyl)cinnolin-4-amine (NEU-1017, 68) for L. major and P. falciparum.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N711 – PubChem

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PROTOZOAN PARASITE GROWTH INHIBITORS

Compounds and methods for inhibiting growth of a protozoan parasite. Methods of treating a protozoan parasite infection in a subject by administering a therapeutically effective amount of a compound as disclosed herein. The compounds and methods can be used to inhibit growth of protozoan parasites such as Trypanosoma brucei, Trypanosoma cruzi, Leishmania spp., and Plasmodium spp.

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Phthalazine – Wikipedia,
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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Late sodium current (late INa) is enhanced during ischemia by reactive oxygen species (ROS) modifying the Nav 1.5 channel, resulting in incomplete inactivation. Compound 4 (GS-6615, eleclazine) a novel, potent, and selective inhibitor of late INa, is currently in clinical development for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia-ventricular fibrillation (VT-VF). We will describe structure-activity relationship (SAR) leading to the discovery of 4 that is vastly improved from the first generation late INa inhibitor 1 (ranolazine). Compound 4 was 42 times more potent than 1 in reducing ischemic burden in vivo (S-T segment elevation, 15 min left anteriorior descending, LAD, occlusion in rabbits) with EC50 values of 190 and 8000 nM, respectively. Compound 4 represents a new class of potent late INa inhibitors that will be useful in delineating the role of inhibitors of this current in the treatment of patients.

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Phthalazine – Wikipedia,
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Application of 152265-57-1, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.152265-57-1, Name is 7-Bromophthalazin-1(2H)-one, molecular formula is C8H5BrN2O. In a article£¬once mentioned of 152265-57-1

INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5), PHARMACEUTICAL PRODUCTS THEREOF, AND METHODS THEREOF

The present invention provides PRMT5 inhibitors of Formula (I), wherein R1 is a non-hydrogen monovalent group; W is a direct bond or -NH-; T, U, and V are independently of each other selected from C and N; R2 is H or a halo; m is 1 or 2; X is a carbon, a nitrogen, or an oxygen; Y is C or N; Z is a direct bond or a carbon; R3 is H, a non-hydrogen monovalent group, an oxo group, a bivalent spiro ring-forming group, or a bivalent bridge-forming group; n is 1 or 2; and Formula (II) stands for a single bond or a double bond. Pharmaceutical products comprising the PRMT5 inhibitors and use thereof in treating proliferative disorders such as cancer, metabolic disorders, blood disorders, autoimmune diseases, and inflammatory diseases are also provided.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N708 – PubChem