Application of (R)-4-(tert-Butoxycarbonyl)thiomorpholine-3-carboxylic acid

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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. 763111-47-3. Here is a downstream synthesis route of the compound 763111-47-3

EXAMPLE A.5. A solution of 4-iodophenyl acetic acid (6.5 mg, 0.048 mmol), EDC (10.5 mg, 0.055 mmol), NHS and 600 mu DMF was stirred for 30 min at room temperature. After this time, the 4-(4-fluoro-3- (piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one (10 mg, 0.0275 mmol) was added to the solution and the mixture was stirred at room temperature overnight. H20 (500 mu) was added, the mixture extracted with DCM (2 x 500 mu), and the combined extracts dried under vacuum. The crude mixture was purified by silica column chromatography (100% DCM), and the product obtained as a white solid (8.8 mg, 61%). 1H NMR (CDCI3) delta = 9.82 (s, 1H), 8.40-8.38 (m, 1H), 7.83-7.81 (d, 1H), 7.77- 7.75 (d, 1H), 7.70-7.69 (m, 2H), 7.63-7.56 (m, 3H), 7.00-6.89 (m, 3H), 4.20 (s, 2H), 3.63-3.11 (m, 8H), 2.84 (s, 2H). LC-ESI-MS (+) m/z = 632.9 [M+Na+]+. HRMS-ESI [M+H+]+ m/z calculated for [C28H24FIN403]+ 611.0955, found 611.0971.

763111-47-3, A chemical reaction often occurs in steps, although it may not always be obvious to an observer. Thank you very much for taking the time to read this article. If you are also interested in other aspects of 763111-47-3, you can also browse my other articles.

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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Research on new synthetic routes about 763111-47-3

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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.

Orapanib intermediate (B) (0.77 kg, 2.10 mol) obtained in step (1) and triethylamine (0.88 kg, 6.32 mol) were added to methylene chloride (5.0 L) and stirred to control temperature 15 CAdd dropwise cyclopropyl carbonyl chloride (0.35L, 3.83mo 1), the dropwise addition, the reaction was stirred at 20-30 C 3h.Add appropriate amount of water, stirring 2h, suction filtration to obtain olaparib (0.79kg, a yield of 87%, a purity of 99.7%).

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.

Reference£º
Patent; Shiyao Group Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.; Wang Liwei; Zhang Hongfen; Zheng Ligang; Ji Dehua; Sun Xiaowei; Yu Pu; Guo Xiaofeng; (8 pag.)CN106928149; (2017); A;,
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Flexible application of 763111-47-3 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

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.

The appropriate acid chloride (0.24 mmol) was added to a solution of 4- [4-Fluoro-3- (piperazine-1-carbonyl) benzyl]-2H-phthalazin-l-one (2) (0.2 mmol) in dichloromethane (2 ml). Hunigs base (0.4 mmol) was then added and the reaction was stirred at room temperature for 16 hours.

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Reference£º
Patent; KUDOS PHARMACEUTICALS LIMITED; MAYBRIDGE LIMITED; WO2004/80976; (2004); A1;,
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The effect of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one reaction temperature change on equilibrium

763111-47-3. 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.

763111-47-3, In the next few decades, the world population will flourish. 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.

A QMA cartridge containing cyclotron -produced [18F] fluoride ion was euted with a solution containing 9 mg Kryptofix [2.2,2] (4,7.13, 16,21,24- hexaoxa- l,10-diaza bicycloi8.8.8]hexacosane), 0.08 m L 0.15 M K2C03 and 1.92 m L MeCN into a 5 m L reaction vial. Water was removed azeotropically at 120 C. 500 mug of ethyl 4-nitrobenzoate dissolved in 100 mu of DMSO was then added to the reaction vial and heated to 150 C for 15 minutes. The reaction via l was then allowed to cool as 50 mu of 1M NaOH was added. The reaction mixture was stirred for 1 min and 50 mu of 1M HCI was added to quench. Then, 2 mg of 4-(4-fiuoro-3-(piperazine-l-carbonyl)benzyi)phthaiazin- l(2H)-one dissolved in 100 mu of DMSO was added , followed by 10 mg of HBT U dissolved in 100 mu of DMSO and 20 mu. of Et3N. The reaction mixture was stirred for 1 minute. 400 mu MeCN followed by 700 mu H20 was then added and the solution was injected onto a C6-Pheny analytical HPLC column and eluted under isocratic conditions (Method B: 30% acetonitrile in water for 35min). Compound C- 2f eluted at (tR = 25.5 min), which was well resolved from the nitro analogue (4-(4-fluoro-3-(4-(4- nitrobenzoyl)piperazine-l-carbonyl)benzyl)phthalazin-l(2H)-one; tR = 30.1 min). For intravenous administration, the product-containing fraction was passed through a CIS light-SepPak cartridge preconditioned with EtOH (10 m L) and water (10 mL). The cartridge was washed with water (3 m L) and C-2f was eluted using EtOH (400 mu). The solution was then diluted with 0.9% saline to 10% EtOH. The radiochemical purity of the final formulation was confirmed using analytical HPLC.

763111-47-3. 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.

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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Rapid Cu-Catalyzed [211At]Astatination and [125I]Iodination of Boronic Esters at Room Temperature

Access to 211At- and 125I-radiolabeled compounds in excellent RCCs and RCYs was achieved in just 10 min at room temperature using a Cu catalyst. The reaction conditions are applicable to a broad class of aryl and heteroaryl boronic reagents with varying steric and electronic properties as well as late-stage astatination and iodination of anticancer PARP inhibitors. This protocol eliminates the traditional need for toxic organotin reagents, elevated temperatures, and extended reaction times, providing a more practical and environmentally friendly approach to developing alpha-emitting radiotherapeutics.

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763111-47-3, Name is 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, belongs to phthalazine compound, is a common compound. SDS of cas: 763111-47-3In an article, once mentioned the new application about 763111-47-3.

Mechanism of Cu-catalyzed aryl boronic acid halodeboronation using electrophilic halogen: Development of a base-catalyzed iododeboronation for radiolabeling applications

An investigation into the mechanism of Cu-catalyzed aryl boronic acid halodeboronation using electrophilic halogen reagents is reported. Evidence is provided to show that this takes place via a boronate-driven ipso-substitution pathway and that Cu is not required for these processes to operate: General Lewis base catalysis is operational. This in turn allows the rational development of a general, simple, and effective base-catalyzed halodeboronation that is amenable to the preparation of 125I-labeled products for SPECT applications.

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of 4-(4-Fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 763111-47-3, in my other articles.

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Red Si-rhodamine drug conjugates enable imaging in GFP cells

Here we evaluated a series of Si-derivatized rhodamine (SiR) dyes for their ability to visualize a model drug in live cells. We show that a charge neutral SiR derivative (but not others) can indeed be used to follow the intracellular location of the model therapeutic drug in GFP cells. This journal is the Partner Organisations 2014.

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An 18F-Labeled Poly(ADP-ribose) Polymerase Positron Emission Tomography Imaging Agent

Poly(ADP-ribose) polymerase (PARP) is involved in repair of DNA breaks and is over-expressed in a wide variety of tumors, making PARP an attractive biomarker for positron emission tomography (PET) and single photon emission computed tomography imaging. Consequently, over the past decade, there has been a drive to develop nuclear imaging agents targeting PARP. Here, we report the discovery of a PET tracer that is based on the potent PARP inhibitor olaparib (1). Our lead PET tracer candidate, [18F]20, was synthesized and evaluated as a potential PARP PET radiotracer in mice bearing subcutaneous glioblastoma xenografts using ex vivo biodistribution and PET-magnetic resonance imaging techniques. Results showed that [18F]20 could be produced in a good radioactivity yield and exhibited specific PARP binding allowing visualization of tumors over-expressing PARP. [18F]20 is therefore a potential candidate radiotracer for in vivo PARP PET imaging.

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RADIOHALIDE-LABELED TARGETED DIAGNOSTICS AND THERAPEUTICS

Disclosed are chemical entities of formula (I) wherein R1, R2 and n are defined herein, and methods of use thereof. These chemical entities are radiative emitters and are useful, e.g., as therapeutic agents for the treatment of, or as diagnostic (e.g., imaging) agents for cancers, e.g., cancers in which PARP1 is overexpressed.

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PHTHALAZINONE DERIVATIVES

Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NR X or CR X R Y ; if X-NR X then n is 1 or 2 and if X-CR X R Y then n is 1; R X is selected from the group consisting of H, optionally substituted C 1-20 alkyl, C 5-20 aryl, C 3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; R Y is selected from H, hydroxy, amino; or R X and R Y may together form a spiro-C 3-7 cycloalkyl or heterocyclyl group; R C1 and R C2 are both hydrogen, or when X is CR X R Y , R C1 , R C2 , R X and R Y , together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R 1 is selected from H and halo

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