Category: 4442-53-9

4442-53-9, In an article, published in an article,authors is Chang, Shaohua, once mentioned the application of 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid,molecular formula is C9H8O4, is a conventional compound. this article was the specific content is as follows.

Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-beta type 1 receptor inhibitors

Inhibition of transforming growth factor beta (TGF-beta) type 1 receptor (ALK5) provides a feasible approach for the treatment of fibrotic diseases and malignant tumors. In this study, we designed and synthesized a new series of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives, and evaluated biologically as TGF-beta type 1 receptor inhibitors. The most potent compound 15r inhibited the ALK5 enzyme and NIH3T3 cell viability with IC50 values of 44 and 42.5 nM, respectively. Compound 15r also displayed better oral plasma exposure and excellent bioavailability than LY-3200882, and in vivo inhibited 65.7% of the tumor growth in a CT26 xenograft mouse model.

4442-53-9, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 4442-53-9

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

4442-53-9, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4. In a Article, authors is Peng, Bo£¬once mentioned of 4442-53-9

Small Molecule Microarray Based Discovery of PARP14 Inhibitors

Poly(ADP-ribose) polymerases (PARPs) are key enzymes in a variety of cellular processes. Most small-molecule PARP inhibitors developed to date have been against PARP1, and suffer from poor selectivity. PARP14 has recently emerged as a potential therapeutic target, but its inhibitor development has trailed behind. Herein, we describe a small molecule microarray-based strategy for high-throughput synthesis, screening of >1000 potential bidentate inhibitors of PARPs, and the successful discovery of a potent PARP14 inhibitor H10 with >20-fold selectivity over PARP1. Co-crystallization of the PARP14/H10 complex indicated H10 bound to both the nicotinamide and the adenine subsites. Further structure?activity relationship studies identified important binding elements in the adenine subsite. In tumor cells, H10 was able to chemically knockdown endogenous PARP14 activities.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.4442-53-9. In my other articles, you can also check out more blogs about 4442-53-9

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

4442-53-9, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 4442-53-9, name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, introducing its new discovery.

THERAPEUTICALLY ACTIVE COMPOUNDS FOR USE IN THE TREATMENT OF CANCER CHARACTERIZED AS HAVING AN IDH MUTATION

Compounds and compositions comprising compounds useful in the treatment of cancer are described herein. The compounds and compositions can be used to modulate an isocitrate dehydrogenase (IDH) mutant (e.g., IDHIm or IDH2m) having alpha hydroxyl neoactivity

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.4442-53-9, you can also check out more blogs about4442-53-9

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

4442-53-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.4442-53-9, Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, molecular formula is C9H8O4. In a Article, authors is Singh, Davinder£¬once mentioned of 4442-53-9

Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR leads to autophosphorylation of receptor tyrosine kinase that initiates a cascade of downstream signaling pathways involved in regulating cellular proliferation, differentiation, and survival. EGFR is abnormally activated by various mechanisms like receptor overexpression, mutation, ligand-dependent receptor dimerization, ligand-independent activation and is associated with the development of variety of human cancers. EGFR inhibition is one of the key targets for cancer chemotherapy. Approval of tyrosine kinase inhibitors such as erlotinib, gefitinib, and lapatinib for the treatment of non-small cell lung cancer led to tremendous development of novel EGFR inhibitors in the last decade. Diverse class of chemical compounds from the synthetic origin has been extensively studied. This review highlights the various classes of synthetically derived molecules which have been reported in the last few years as potential EGFR and EGFR/ErbB-2 dual inhibitors. A brief synthetic methodology to access these compounds has been highlighted along with the SAR. We strongly believe that this review will provide a platform to the synthetic chemists and biologists to design and synthesize new and potent compounds that inhibit EGFR and ErbB-2.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.4442-53-9. In my other articles, you can also check out more blogs about 4442-53-9

Reference£º
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

4442-53-9, 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. 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, cas is 4442-53-9,the benzodioxans compound, it is a common compound, a new synthetic route is introduced below.

Example 81a (S)-ethyl 4-amino-5-(2-(2,3-dihydrobenzo[b][1,4]dioxine-5-carboxamido)-propoxy)-2-methylquinoline-3-carboxylate Prepared as in Example 24a from (S)-ethyl 4-amino-5-(2-aminopropoxy)-2-methyl-quinoline-3-carboxylate (Example 26b) and 2,3-dihydrobenzo[b][1,4]dioxine-5-carboxylic acid as brown solid. MS 466 (MH+).

The chemical industry reduces the impact on the environment during synthesis,4442-53-9,2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid,I believe this compound will play a more active role in future production and life.

Reference£º
Patent; SENOMYX, INC.; US2012/41078; (2012); A1;,
Benzodioxan
1,4-Benzodioxane | C8H8O2 – PubChem

Name is 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, as a common heterocyclic compound, it belongs to benzodioxans compound, and cas is 4442-53-9, its synthesis route is as follows.

Example 106a (S)-ethyl 4-amino-5-(2-(2,3-dihydrobenzo[b][1,4]dioxine-5-carboxamido)-3-methylbutoxy)-2-methylquinoline-3-carboxy late Prepared as in Example 24a from (S)-ethyl 4-amino-5-(2-amino-3-methylbutoxy)-2-methylquinoline-3-carboxylate (Example 95b) and 2,3-dihydrobenzo[b][1,4]dioxine-5-carboxylic acid as brown solid (36%). MS 494 (MH+).

4442-53-9, 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.,4442-53-9 ,2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, other downstream synthetic routes, hurry up and to see

Reference£º
Patent; SENOMYX, INC.; US2012/41078; (2012); A1;,
Benzodioxan
1,4-Benzodioxane | C8H8O2 – PubChem

2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, cas is 4442-53-9, it is a common heterocyclic compound, the benzodioxans compound, its synthesis route is as follows.,4442-53-9

Example 99a(S)-ethyl 4-amino-5-(2-(2,3-dihydrobenzo[b][1,4]dioxine-5-carboxamido)-butoxy)-2-methylquinoline-3-carboxylatePrepared as in Example 24a from (S)-ethyl 4-amino-5-(2-aminobutoxy)-2-methylquinoline-3-carboxylate (Example 97b) and 2,3-dihydrobenzo[b][1,4]dioxine-5-carboxylic acid as brown solid (40percent). MS 480 (MH+).

With the rapid development of chemical substances, we look forward to future research findings about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

Reference£º
Patent; SENOMYS, INC.; US2011/245353; (2011); A1;,
Benzodioxan
1,4-Benzodioxane | C8H8O2 – PubChem

2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, cas is 4442-53-9, it is a common heterocyclic compound, the benzodioxans compound, its synthesis route is as follows.,4442-53-9

6,7-dibromo-1,4 -benzodioxane-5-carboxylic acid 1,440 ml of acetic acid and 360 g of 1,4-benzodioxane-5-carboxylic acid were introduced into a balloon flask provided with an agitator, an introduction funnel and a condenser. The mixture was heated to 55¡ã C. and then a solution of 700 g of bromine in 360 ml of acetic acid was added in portions. The mixture was heated to 120¡ã C. and then cooled to 15¡ã C. The precipitate was dried off, washed with acetic acid and dried. 332 g of 6,7-dibromo-1,4-benzodioxane-5-carboxylic acid were obtained (M.P.: 212¡ã C.). The structure was confirmed by nuclear magnetic resonance analysis.

4442-53-9 is used more and more widely, we look forward to future research findings about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

Reference£º
Patent; Societe D’Etudes Scientifiques et Industrielles de L’ile-de-France; US4186135; (1980); A;,
Benzodioxan
1,4-Benzodioxane | C8H8O2 – PubChem

It is a common heterocyclic compound, the benzodioxans compound, 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, cas is 4442-53-9 its synthesis route is as follows.,4442-53-9

At room temperature, diphenyl phosphoryl azide (8.02g, 29mmol) and triethyl amine (4.2g, 42mmol) were added to a solution of 2,3-dihydro-1,4-benzodioxane-5-carboxylic acid (5.0g, 28mmol) in anhydrous THF (110mL). The mixture was stirred for 2hrs, followed by adding water (30mL), heating to 70 ¡ãC and further reacting for 3hrs, then cooling to room temperature, being extracted with EA (100mL*3). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure. The residue was purified by silica column chromatography (PE:EA = 5:1) to give compound 11-f (1.58g, yield 37percent). LC-MS (ESI): m/z = 152 [M+H]+.

With the complex challenges of chemical substances, we look forward to future research findings about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

Reference£º
Patent; Shanghai Yingli Pharmaceutical Co. Ltd.; XU, Zusheng; ZHANG, Nong; SUN, Qingrui; WU, Tianzhi; (104 pag.)EP3275867; (2018); A1;,
Benzodioxan
1,4-Benzodioxane | C8H8O2 – PubChem

2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid, cas is 4442-53-9, it is a common heterocyclic compound, the benzodioxans compound, its synthesis route is as follows.,4442-53-9

4.1.1.1. 6-Bromo-3-((2,3-dihydrobenzo[b][1,4]dioxin-5-yl)methyl)-2-methoxyquinoline (VI: Y = 2,3-O(CH2)2O-). To a solution of 2,3-dihydrobenzo[b][1,4]dioxine-5-carboxylic acid (5.00 g, 28.0 mmol)in THF (150 mL) at 0 C was added lithium aluminium hydride(2.13 g, 56.0 mmol) in small portions. The reaction mixture wasstirred at 0 C for 10 min and stirred for a further 18 h at 20 C.Water (150 mL) was added to the reaction mixture which wasextracted with EtOAc (2 100 mL). The combined organic layerswere washed with brine (100 mL), dried over Na2SO4, filteredand concentrated under reduced pressure to obtain (2,3-dihydrobenzo[b][1,4]dioxin-5-yl)methanol as a yellow oil (3.22 g,99%). 1H NMR (CDCl3, 400 MHz) d 6.87-6.79 (m, 3H), 4.66 (s, 2H),4.32-4.30 (m, 2H), 4.28-4.25 (m, 2H), 2.19 (bs, 1H). Found: [M+H-18] = 149.5.

With the rapid development of chemical substances, we look forward to future research findings about 2,3-Dihydrobenzo[b][1,4]dioxine-5-carboxylic acid

Reference£º
Article; Sutherland, Hamish S.; Tong, Amy S.T.; Choi, Peter J.; Conole, Daniel; Blaser, Adrian; Franzblau, Scott G.; Cooper, Christopher B.; Upton, Anna M.; Lotlikar, Manisha U.; Denny, William A.; Palmer, Brian D.; Bioorganic and Medicinal Chemistry; vol. 26; 8; (2018); p. 1797 – 1809;,
Benzodioxan
1,4-Benzodioxane | C8H8O2 – PubChem