Category: 74704-39-5

Phthalazinone Pyrazoles as Potent, Selective, and Orally Bioavailable Inhibitors of Aurora-A Kinase was written by Prime, Michael E.;Courtney, Stephen M.;Brookfield, Frederick A.;Marston, Richard W.;Walker, Victoria;Warne, Justin;Boyd, Andrew E.;Kairies, Norman A.;von der Saal, Wolfgang;Limberg, Anja;Georges, Guy;Engh, Richard A.;Goller, Bernhard;Rueger, Petra;Rueth, Matthias. And the article was included in Journal of Medicinal Chemistry in 2011.Electric Literature of C5H6BrNS The following contents are mentioned in the article:

The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacol. profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Electric Literature of C5H6BrNS).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Electric Literature of C5H6BrNS

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Total Syntheses of Epothilones B and D was written by Jung, Jae-Chul;Kache, Rajashaker;Vines, Kimberly K.;Zheng, Yan-Song;Bijoy, Panicker;Valluri, Muralikrishna;Avery, Mitchell A.. And the article was included in Journal of Organic Chemistry in 2004.Recommanded Product: 4-(Bromomethyl)-2-methylthiazole The following contents are mentioned in the article:

A convergent, total synthesis of epothilones B (I; X = O) and D (I; X = bond) is described. The key steps are Normant coupling to establish the desired (Z)-stereochem. at C12-C13, Wadsworth-Emmons olefination, diastereoselective aldol condensation of aldehyde II with the enolate of keto acid derivatives to form the C6-C7 bond, selective deprotection, and macrolactonization. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Recommanded Product: 4-(Bromomethyl)-2-methylthiazole).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Recommanded Product: 4-(Bromomethyl)-2-methylthiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Discovery of a New Class of Potent, Selective, and Orally Bioavailable CRTH2 (DP2) Receptor Antagonists for the Treatment of Allergic Inflammatory Diseases was written by Crosignani, Stefano;Page, Patrick;Missotten, Marc;Colovray, Veronique;Cleva, Christophe;Arrighi, Jean-Francois;Atherall, John;Macritchie, Jackie;Martin, Thierry;Humbert, Yves;Gaudet, Marilene;Pupowicz, Doris;Maio, Maurizio;Pittet, Pierre-Andre;Golzio, Lucia;Giachetti, Claudio;Rocha, Cynthia;Bernardinelli, Gerald;Filinchuk, Yaroslav;Scheer, Alexander;Schwarz, Matthias K.;Chollet, Andre. And the article was included in Journal of Medicinal Chemistry in 2008.Computed Properties of C5H6BrNS The following contents are mentioned in the article:

A novel chem. class of potent chemoattractant receptor-homologous expressed on Th2 lymphocytes (CRTH2 or DP2) antagonists is reported. An initial and moderately potent spiro-indolinone compound (I) was found during a high-throughput screening campaign. Structure-activity relationship (SAR) investigation around the carboxylic acid group revealed that changes in this part of the mol. could lead to a reversal of functional activity, yielding weakly potent agonists. SAR investigation of the succinimide functional group led to the discovery of several single-digit nanomolar antagonists. The potency of these compounds was confirmed in a human eosinophil chemotaxis assay. Moreover, compounds II and III were shown to possess pharmacokinetic properties suitable for development as an orally bioavailable drug. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Computed Properties of C5H6BrNS).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Computed Properties of C5H6BrNS

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Cyclopropanation of 3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-diones was written by Lack, Oliver;Martin, Rainer E.. And the article was included in Tetrahedron Letters in 2005.Related Products of 74704-39-5 The following contents are mentioned in the article:

A two step parallel synthesis protocol for the preparation of 1N-substituted spirobenzodiazepineones is described. Treatment of 4-methyl-3,4-dihydro-1H-benzo[e][1,4]diazepine-2,5-dione with a series of alkyl halides using a microwave-assisted heating protocol provided N-derivatized compounds, which were transformed to the corresponding cyclopropylamines employing modified Kulinkovich-type reaction conditions. X-ray structural anal. gave conclusive evidence of the newly created spiro center and revealed a significant flattening of the seven-membered ring system compared with the benzodiazepinedione system providing a characteristically different pattern of bond exit vectors. The physicochem. parameters log D, pK_a, solubility, and membrane permeability of both cyclopropanated and precursor compounds were assessed. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Related Products of 74704-39-5).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Related Products of 74704-39-5

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

12,13-Aziridinyl Epothilones. Stereoselective Synthesis of Trisubstituted Olefinic Bonds from Methyl Ketones and Heteroaromatic Phosphonates and Design, Synthesis, and Biological Evaluation of Potent Antitumor Agents was written by Nicolaou, K. C.;Rhoades, Derek;Wang, Yanping;Bai, Ruoli;Hamel, Ernest;Aujay, Monette;Sandoval, Joseph;Gavrilyuk, Julia. And the article was included in Journal of the American Chemical Society in 2017.Name: 4-(Bromomethyl)-2-methylthiazole The following contents are mentioned in the article:

The synthesis and biol. evaluation of a series of 12,13-aziridinyl epothilone B analogs is described. These compounds were accessed by a practical, general process that involved a 12,13-olefinic Me ketone as a starting material obtained by ozonolytic cleavage of epothilone B followed by tungsten-induced deoxygenation of the epoxide moiety. The attachment of the aziridine structural motif was achieved by application of the Ess-Kurti-Falck aziridination, while the heterocyclic side chains were introduced via stereoselective phosphonate-based olefinations. In order to ensure high (E) selectivities for the latter reaction for electron-rich heterocycles, it became necessary to develop and apply an unprecedented modification of the venerable Horner-Wadsworth-Emmons reaction, employing 2-fluoroethoxyphosphonates that may prove to be of general value in organic synthesis. These studies resulted in the discovery of some of the most potent epothilones reported to date. Equipped with functional groups to accommodate modern drug delivery technologies, some of these compounds exhibited picomolar potencies that qualify them as payloads for antibody drug conjugates (ADCs), while a number of them revealed impressive activities against drug resistant human cancer cells, making them desirable for potential medical applications. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Name: 4-(Bromomethyl)-2-methylthiazole).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Name: 4-(Bromomethyl)-2-methylthiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica