Category: 4771-48-6

Duguta, Govardhan; Muddam, Bhooshan; Kamatala, Chinna Rajanna; Chityala, Yadaiah published the artcile< Symmetric trichloro triazine adducts with N, N'-dimethyl formamide and N, N'-dimethyl acetamide as green Vilsmeier -Haack reagents for effective formylation and acylation of Indoles>, Electric Literature of 4771-48-6, the main research area is trichloroisocyanuric acid dimethyl formamide indole formylation acetylation Vilsmeier Haack; indolecarbaldehyde acetylindole green chem.

Sym. trichloro triazine (trichlorotriazine (TCTA), and trichloroisocyanuric acid (TCCA)) adducts with N, N’-dimethyl formamide (DMF) N, N’-dimethyl acetamide (DMA) were explored as green Vilsmeier -Haack (VH) reagents for effective formylation and acetylation of indole. Reaction times (RT) reduced significantly in (TCTA/DMF), (TCCA/DMF), (TCTA/DMA) and (TCCA/DMA) triggered reactions followed by yield increments. Microwave assisted (MWA) protocols with these reagents reduced the reaction times from several hours to only few minutes followed by yield enhancements.

Chemical Data Collections published new progress about Acetylation. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Electric Literature of 4771-48-6.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Xu, Hui; Wang, Yang-Yang published the artcile< Antifungal agents. Part 5: Synthesis and antifungal activities of aminoguanidine derivatives of N-arylsulfonyl-3-acylindoles>, Safety of 4-Methyl-1H-indole-3-carbaldehyde, the main research area is arylsulfonylacylindole aminoguanidine preparation antifungal structure activity relationship.

In order to discover more promising antifungal agents, a series of aminoguanidine derivatives of N-arylsulfonyl-3-acylindoles were prepared and evaluated in vitro for their antifungal activities against seven phytopathogenic fungi. Some of the compounds exhibited more potent antifungal activities than or comparable to hymexazol, a com. available agricultural fungicide at the concentration of 100 μg/mL. Preliminary structure-activity relationships of antifungal activities were investigated.

Bioorganic & Medicinal Chemistry Letters published new progress about Fungicides. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Safety of 4-Methyl-1H-indole-3-carbaldehyde.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wang, Qinghui; Arnst, Kinsie E.; Wang, Yuxi; Kumar, Gyanendra; Ma, Dejian; Chen, Hao; Wu, Zhongzhi; Yang, Jinliang; White, Stephen W.; Miller, Duane D.; Li, Wei published the artcile< Structural Modification of the 3,4,5-Trimethoxyphenyl Moiety in the Tubulin Inhibitor VERU-111 Leads to Improved Antiproliferative Activities>, Related Products of 4771-48-6, the main research area is trimethoxyphenyl VERU111 synthesis tubulin antitumor.

Colchicine binding site inhibitors (CBSIs) hold great potential in developing new generations of antimitotic drugs. Unlike existing tubulin inhibitors such as paclitaxel, they are generally much less susceptible to resistance caused by the overexpression of drug efflux pumps. The 3,4,5-trimethoxyphenyl (TMP) moiety is a critical component present in many CBSIs, playing an important role in maintaining suitable mol. conformations of CBSIs and contributing to their high binding affinities to tubulin. Previously reported modifications to the TMP moiety in a variety of scaffolds of CBSIs have usually resulted in reduced antiproliferative potency. We previously reported a potent CBSI, VERU-111, that also contains the TMP moiety. Herein, we report the discovery of a VERU-111 analog I that is significantly more potent than VERU-111. The X-ray crystal structure of I in complex with tubulin confirms its direct binding to the colchicine site. In addition, I exhibited a strong inhibitory effect on tumor growth in vivo.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Related Products of 4771-48-6.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Lu, Lin; Zheng, Zuoliang; Yang, Yongjie; Liu, Bo; Yin, Biaolin published the artcile< Access to Polycyclic Indol(en)ines via Base-Catalyzed Intramolecular Dearomatizing 3-Alkenylation of Alkynyl Indoles>, Reference of 4771-48-6, the main research area is indolylmethylpropynamide sodium methoxide catalyst diastereoselective regioselective dearomatization alkenylation spirocyclization; methylidene spiroindolepyrrolidinone preparation; methylidenyl dihydrospiroindolepyrrolidinone preparation; carbamoyl indolylmethylpropynamide sodium methoxide catalyst dearomatization alkenylation cyclization; tetrahydropyrrolopyrroloindole dione preparation diastereoselective regioselective.

Polycyclic indolines and indolenines were synthesized via base-catalyzed intramol. dearomatizing 3-alkenylation reactions of alkynyl indoles at room temperature The base enhanced the nucleophilicity of the carbon at the 3-position of the indole moiety, facilitating an exclusive 5-exo-dig cyclization reaction with the alkyne to form spiroindolenines I, III [R3 = Et, Pr, iso-Pr, etc]. The imine functionality of spiroindolenines I was undergo in-situ nucleophilic addition to form spiroindolines II [R1 = H, 4-Me, 5-Cl, etc.; R2 = Ph, 2-methylphenyl, 3-methylphenyl; R3 = Pr, benzyl, 4-methoxyphenyl; R4 = tert-Bu, cyclohexyl] when R was a carbamoyl group or reduction to form spiroindolines III when R was H.

Chinese Journal of Chemistrypublished new progress about Alkenes Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Reference of 4771-48-6.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Lin, Hui-Shan; Chen, Shu-Jun; Huang, Jing-Mei published the artcile< Electrosynthesis of (hetero)aryl nitriles from α-imino-oxy acids via oxidative decarboxylation/N-O cleavage>, Synthetic Route of 4771-48-6, the main research area is indolylemthyliminooxy acid electrochem oxidative decarboxylation cleavage; indolyl carbonitrile preparation.

A new method for the synthesis of (hetero)aryl nitriles via iminyl radicals was developed through the electrochem. oxidative decarboxylation of α-imino-oxy acids. This protocol provides an efficient approach to nitriles with a broad range of functional-group tolerance under ambient conditions and can be applied for one-pot gram-scale synthesis.

Chemical Communications (Cambridge, United Kingdom)published new progress about Aromatic nitriles Role: SPN (Synthetic Preparation), PREP (Preparation). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Synthetic Route of 4771-48-6.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Wang, Zhao-Yang; Guo, Rui-Li; Zhang, Xing-Long; Wang, Meng-Yue; Chen, Gang-Ni; Wang, Yong-Qiang published the artcile< Regioselective C5-H direct iodination of indoles>, COA of Formula: C10H9NO, the main research area is iodo indole regioselective preparation; aryl iodide iodosuccinimide iodination.

An efficient regioselective C5-H direct iodination of indoles I [R = H, 6-Cl, 4-Me, etc.; R1 = C(O)H, CN, C(O)OMe, C(O)OEt] was developed for the first time. Due to the versatility of aryl iodides, the method offered a general and practical access to the C5 functionalization of indoles. The approach featured mild reaction conditions, good tolerance of functional groups and more crucially, no metal involved in the reaction, thereby benefitting the late-stage decoration of medicinal mols. A mechanistic study showed that the current iodination reaction proceeded via a radical pathway.

Organic Chemistry Frontierspublished new progress about Aryl iodides Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, COA of Formula: C10H9NO.

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4771-48-6,4-Methyl-1H-indole-3-carbaldehyde,as a common compound, the synthetic route is as follows.

The intermediate 1- (3,4,5-trimethoxyphenyl) propan-1-one (448 mg, 2 mmol) was dissolved in a solution of piperidine (0.1 mL) in toluene (6 mL), and 4-methyl-1H-indole-3-carboxaldehyde (156.8mg, 0.8mmol), reacted at 130 C for 4h,The organic phase was spin-dried, and the remaining crude product was recrystallized from ethanol to obtain the target compound (E)-2-methyl-3-(4-methyl-1H-indol-3-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (1) 230mg,The yield was 51.3%.

4771-48-6, 4771-48-6 4-Methyl-1H-indole-3-carbaldehyde 2762437, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; Ningxia Medical University; Zhuang Chunlin; Shi Ying; Cong Hui; Zhang Wannian; Huang Jiaxuan; Yu Jianqiang; Xu Lijuan; Qu Zhuo; (21 pag.)CN110526854; (2019); A;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles