763111-47-3 | Heterocyclic Building Blocks-phthalazine

Research on new synthetic routes about 763111-47-3

The chemical industry reduces the impact on the environment during synthesis,763111-47-3,4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one,I believe this compound will play a more active role in future production and life.

The molecularity of an elementary reaction is the number of molecules that collide during that step in the mechanism. 763111-47-3, If there is only a single reactant molecule in an elementary reaction, that step is designated as unimolecular.4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound. A new synthetic method of this compound is introduced below.

4-(4-Fluoro-3-(piperazin-1-yl-carbonyl)-benzyl)pyridazine-1(2H)one (5) (1.56 g, 4.26 mmol) was added to a 25 ml three-necked flask.And added dichloromethane (6.5 ml), trans-4-dimethylamino crotonic acid (0.78 g, 6.04 mmol),HOBT (0.87 g, 6.44 mmol), EDCI (1.23 g, 6.42 mmol), and then cooled to 0-10 C, then DIPEA (4.42 g, 34.3 mmol) was added dropwise, and the mixture was allowed to warm to room temperature and stirred for 2 h.After TLC showed that the reaction was completed, the reaction mixture was quenched with water (30 mL).The solid crude product was added to the acid water, the impurities were extracted with dichloromethane, the aqueous phase was made alkaline, and the product was extracted with dichloromethane (20 mL¡Á3);The combined organic phases were dried over anhydrous sodium sulfate, filtered and evaporatedThe white solid product was then beaten with n-hexane (5 ml).Filter and dry to give 470 mg of a white solid.The yield was 23%.

Reference£º
Patent; Shanghai Bobang Pharmaceutical Technology Co., Ltd.; Gao Heyong; Liu Zhende; Zhang Wensheng; (28 pag.)CN108383798; (2018); A;,
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Share a compound : 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, 763111-47-3

In the next few decades, the world population will flourish. 763111-47-3.As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound, it is a common compound, a new synthetic route is introduced below.

To the reaction kettle was added 6 L of dichloromethane,4- (4-fluoro-3- (piperazine-1-carbonyl) benzyl) phthalazin-1 (2-hydro) -one (400 g, 1.09 mol)Cooled to 0 C,Triethylamine (153 g, 210 mL, 1.51 mol) was slowly added,Cyclopropanecarbonyl chloride (130 g, 1.24 mol)Stir at room temperature,After TLC detection reaction,Add 3L of water,2L dichloromethane,Dispensing,The organic phase was removed by distillation under reduced pressure,To obtain 320 g of a yellow solid;HPLC purity 96.13%Yield 67.5%.

Reference£º
Patent; Sichuan Kelun Drug Research Institute Co., Ltd.; Li, Hongming; Wu, Wei; Tuo, Shichuan; Wang, Lichun; Wang, Jingyi; (8 pag.)CN105985294; (2016); A;,
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The effect of 763111-47-3 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.763111-47-3, 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. 763111-47-3, name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, introduce a new downstream synthesis route as follows. 763111-47-3

To 20 mg (54.5 muiotaetaomicronIota) of 4-(4-fluoro-3-(piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one dissolved in 1 mL of MeCN, 9.2 mg (65.5 muiotaetaomicronIota) 4-fluorobenzoic acid was added followed by 24.8 mg (65.5 muiotaetaomicronIota) of HBTU and 18 mu (131 muiotaetaomicronIota) of Et3N. The reaction mixture was stirred for 5 minutes and purified by H PLC to yield the compound as an orange solid (11.5 mg, 23.5 muiotaetaomicronIota, 43%). 1H-NM R (500 M Hz, CDC delta = 10.74 (s, 1H), 8.51-8.49 (d, 1H), 7.83-7.76 (m, 2H), 7.82 (s, 1H), 7.45-7.44 (m, 2H), 7.38-7.36 (m, 2H), 7.14-7.08 (m, 3H), 4.33 (s, 2H), 3.75-3.39 (m, 8H). MS-ES m/z [M + Na]+ = 511.2. H RMS-ESi m/z calculated for [C27 H22 N4 03 F2 Naf 511.1558, found 511.1569 [M + Na]+.

Reference£º
Patent; MEMORIAL SLOAN KETTERING CANCER CENTER; REINER, Thomas; LEWIS, Jason S.; WEBER, Wolfgang; RODRIGUEZ, Beatriz Salinas; CARNEY, Brandon; CARLUCCI, Giuseppe; (89 pag.)WO2016/33293; (2016); A1;,
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Flexible application of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one in synthetic route

763111-47-3, There are, however, a few established termolecular elementary reactions. The reaction of nitric oxide with oxygen appears to involve termolecular steps. you can also browse my other articles about 763111-47-3

Rate laws may be derived directly from the chemical equations for elementary reactions. This is not the case, however, for ordinary chemical reactions.4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound, below Introduce a new synthetic route., 763111-47-3

An appriopriate aldehyde (0.2 mmol) and 4- [4-FLUORO-3- (PIPERAZINE-L- carbonyl) BENZYL]-2H-PHTHALAZIN-1-ONE (2) (0.24 mmol) were dissolved in dichloromethane (2 ml). Sodium triacetoxyborohydride (0.28 mmol) and glacial acetic acid (6.0 mmol) were then added and stirred at room temperature for 16 hours. The reaction mixtures were then purified by preparative HPLC.

Reference£º
Patent; KUDOS PHARMACEUTICALS LIMITED; MAYBRIDGE LIMITED; WO2004/80976; (2004); A1;,
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Flexible application of 763111-47-3 in synthetic route

763111-47-3, Rate laws may be derived directly from the chemical equations for elementary reactions. This is not the case, however, for ordinary chemical reactions.4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound, below Introduce a new synthetic route.

Step 3: Preparation of 4-(4-fluoro-3-(4-(2-methyl-2-((5-(trifluoromethyl) pyridin-2- yl)oxy) propanoyl)piperazine-l-carbonyl) benzyl) phthalazin-l(2H)-one.To a solution of 2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanoic acid (0.204 g, 0.81 mmol) in dry DMF (6 mL) was added TBTU (0.289 g, 0.90 mmol) at room temperature under atmosphere of nitrogen. To this 4-(4-fluoro-3-(piperazine-l- carbonyl)benzyl)phthalazin-l(2H)-one (0.3 g, 0.81 mmol) and DIPEA (0.303 mL, 1.74 mmol) were added. The reaction mixture was stirred at room temperature for 2 h. The progress of reaction was checked by TLC by using mobile phase 5 % methanol in chloroform. The reaction mixture was diluted with ethyl acetate. The organic layer was washed with water, dried over anhydrous Na2S04 and solvents were evaporated on a rotatory evaporator under reduced pressure to crude solid which was purified by the flash column chromatography using eluent chloroform : methanol (98.3 : 1.7) to afford 4-(4-fluoro-3-(4-(2-methyl-2-((5-(trifluoromethyl) pyridin-2-yl)oxy) propanoyl)piperazine-l-carbonyl) benzyl) phthalazin-l(2H)-one as white solid (0.230 g, 47 %).

Reference£º
Patent; CADILA HEALTHCARE LIMITED; SHRIVASTAVA, Brijesh Kumar; WO2012/14221; (2012); A1;,
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Research on new synthetic routes about 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

763111-47-3, In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles.,763111-47-3 ,4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, other downstream synthetic routes, hurry up and to see

One of the major reasons is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time, to discover the sequence of events that occur at the molecular level.4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound, introduce a new downstream synthesis route. 763111-47-3

EXAM PLE A.2. Compound c-1 (127l): 4-(4-fluoro-3-(4-(3-iodobenzoyl)piperazine-l-carbonyl)benzyl)- phthalazin-l(2H)-one. (0301) [0148] To a solution of 4-(4-fluoro-3-(piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one (10 mg, 0.0275 mmol), triethylamine (40 mu, 0.3 mmol) a nd H BTU (16 mg, 0.0413 mmol) in dimethyl formamide (DM F, 500 mu) was added to 3-iodobenzoic acid (6 mg, 0.0275 mmol). The mixtu re was stirred at room temperature for 20 h. The crude product was then purified by preparative HPLC and dried under vacuum, yielding a white solid (6.9 mg, 48% yield). 1H NM R (CDCIs) delta = 10.00 (s, 1H), 8.40-8.38 (m, 1H), 7.71-7.69 (m, 4H), 7.64-7.63 (m, 1H), 7.30-7.26 (m, 3H), 7.09 (m, 1H), 7.04-6.87 (m, 1H), 4.21 (s, 2H), 3.71-3.29 (m, 8H). LC-ESI-MS (+) m/z = 597.1 [M+H+]+. H RMS-ESI [M-H+]” m/z calculated for [C27H22FIN4O3]- 595.0642, found 595.0660.

Discovery of 763111-47-3

4-[[4-Fluoro-3-(piperazine-1-carbonyl)phenyl]methyl]-2H-phthalazin-1-one (11) (86 mg, 0.24 mmol), HBTU (116 mg, 0.30 mmol) and triethylamine (164 muL, 1.18 mmol) were added to a solution of 2-hydroxyacetic acid (36 mg, 0.48 mmol) in DMF (1.5 mL) and the reaction mixture was stirred at room temperature for 40 minutes, before dichloromethane (4 mL) and water (4 mL) were added, the organic phase separated and washed with NaOH (0.2 M, 3*4 mL) and water (3*4 mL). The organic phase was dried over MgSO4, volatiles were removed in vacuo and the resulting crude material was purified via HPLC, yielding the title compound as a clear solid (24.3 mg, 0.06 mumol, 50%).

Reference£º
Patent; THE GENERAL HOSPITAL CORPORATION; Reiner, Thomas; Keliher, Edmund J.; Weissleder, Ralph; US2013/309170; (2013); A1;,
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The effect of the change of 763111-47-3 synthetic route on the product

A balanced equation for a chemical reaction indicates what is reacting and what is produced, but it reveals nothing about how the reaction actually takes place. The reaction mechanism is the process, or pathway, by which a reaction occurs.4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound. An updated downstream synthesis route of 763111-47-3 as follows. 763111-47-3

4-(4-Fluoro-3-(piperazin-1-yl-carbonyl)-benzyl)pyridazine-1(2H)one (5) (0.78 g, 2.13 mmol) was added to a 25 ml three-necked flask.Dichloromethane (6.5 ml) and triethylamine (0.52 g, 5.14 mmol) were added, and the mixture was stirred and cooled to 1-10 C.Further, 2-butenyl chloride (268 mg, 2.56 mmol) was added dropwise, and the mixture was warmed to room temperature and stirred for 1 hour.TLC showed the reaction was complete; the reaction mixture was directly concentrated to dryness, and the residue was mixed with water and then stirred for 1 hour and then filtered.Obtained as an off-white solid.The yield was 37%.

The influence of catalyst in 763111-47-3 reaction

763111-47-3, An elementary termolecular reaction involves the simultaneous collision of three atoms, molecules, or ions.4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound. Here is a downstream synthesis route of the compound 763111-47-3

4-(4-Fluoro-3-(piperazin-1-yl-carbonyl)-benzyl)pyridazine-1(2H)one (5) (0.78 g, 2.13 mmol) was added to a 25 ml three-necked flask.And adding dichloromethane (6.5 ml), 2-butynoic acid (215 mg, 2.56 mmol), HOBT (431 mg, 3.20 mmol), EDCI (614 mg, 3.20 mmol), and stirring to 1-10 C,An excess of DIPEA (550 mg, 4.26 mmol) was added dropwise and the mixture was allowed to warm to room temperature.After TLC showed that the reaction was completed, the reaction mixture was directly concentrated to dryness, and the residue was mixed with water and then stirred for 1 hour and then filtered.Obtained as an off-white solid.The yield was 31%.

Derivation of elementary reaction about 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one

The molecularity of an elementary reaction is the number of molecules that collide during that step in the mechanism. If there is only a single reactant molecule in an elementary reaction, that step is designated as unimolecular.4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, cas is 763111-47-3,the phthalazine compound. A new synthetic method of this compound is introduced below. 763111-47-3

4,4′-(((4,4′-(4,4′-(1,1,3,3-tetramethyldisiloxane-1,3-diyl)bis(butanoyl))bis(piperazine-4,1- diyl-1-carbonyl))bis(4-fluoro-3,1-phenylene))bis(methylene))bis(phthalazin-1(2H)-one): (0224) [3]: (0225) [00132] A solution of 4,4′-(1,1,3,3-tetramethyldisiloxane-1,3-diyl)dibutyric acid (250 mg, 0.816 mmol) in dichlromethane(5 mL) was charged EDCI-HCl (396 mg, 2.042 mmol) and 4-(4-fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one (598 mg, 1.633 mmol) at room temperature and stirred for 1hh. After completion of the reaction (monitored by TLC), water (5 mL) was added in the reaction mixture and organic layer was separated to obtain crude compound. The crude compound was purified by CombiFlash chromatography using 1-10% MeOH in DCM to obtain 286mg, 38% yield of the title compound as an off white solid.1H NMR (400 MHz, DMSO-d6): delta 12.57 (s, 2H), 8.55 (d, J = 10.27 Hz, 2H), 8.23 (d, J = 7.83 Hz, 1H), 7.92-7.96 (m, 1H), 7.84-7.89 (m, 2H), 7.78-7.83 (m, 2H), 7.38-7.44 (m, 2H), 7.33 (br. s, 2H), 7.21 (t, J = 8.80 Hz, 2H), 4.44 (s, 2H), 4.30 (s, 2H), 3.49-3.62 (m, 14H), 3.33-3.38 (m, 4H), 3.08-3.18 (m, 2H), 2.25-2.38 (m, 4H), 1.44-1.55 (m, 2H), 0.46-0.54 (m, 2H), 0.14 (br. s, 3H), 0.13 (br. s, 3H), 0.04 (br. s, 3H), 0.03 (br. s, 3H); MS (ES+): m/z = 493.20 [Monomer M – 18]+; LCMS: tR = 0.792 min.

Reference£º
Patent; BLINKBIO, INC.; WANNER, Jutta; NGUYEN, Hanh, Nho; WERNER, Douglas, S.; OFORI, Leslie, Odame; (167 pag.)WO2017/214491; (2017); A1;,
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