Tag: 100-200

The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity was written by Newton, Rebecca;Bowler, Katherine A.;Burns, Emily M.;Chapman, Philip J.;Fairweather, Emma E.;Fritzl, Samantha J. R.;Goldberg, Kristin M.;Hamilton, Niall M.;Holt, Sarah V.;Hopkins, Gemma V.;Jones, Stuart D.;Jordan, Allan M.;Lyons, Amanda J.;Nikki March, H.;McDonald, Neil Q.;Maguire, Laura A.;Mould, Daniel P.;Purkiss, Andrew G.;Small, Helen F.;Stowell, Alexandra I. J.;Thomson, Graeme J.;Waddell, Ian D.;Waszkowycz, Bohdan;Watson, Amanda J.;Ogilvie, Donald J.. And the article was included in European Journal of Medicinal Chemistry in 2016.Recommanded Product: 5-Amino-2,4-dichlorophenol This article mentions the following:

Deregulation of the receptor tyrosine kinase RET has been implicated in medullary thyroid cancer, a small percentage of lung adenocarcinomas, endocrine-resistant breast cancer and pancreatic cancer. There are several clin. approved multi-kinase inhibitors that target RET as a secondary pharmacol. but addnl. activities, most notably inhibition of KDR, lead to dose-limiting toxicities. There is, therefore, a clin. need for more specific RET kinase inhibitors. Herein we report our efforts towards identifying a potent and selective RET inhibitor using vandetanib 1 as the starting point for structure-based drug design. Phenolic anilinoquinazolines exemplified by 6 showed improved affinities towards RET but, unsurprisingly, suffered from high metabolic clearance. Efforts to mitigate the metabolic liability of the phenol led to the discovery that a flanking substituent not only improved the hepatocyte stability, but could also impart a significant gain in selectivity. This culminated in the identification of 36; a potent RET inhibitor with much improved selectivity against KDR. In the experiment, the researchers used many compounds, for example, 5-Amino-2,4-dichlorophenol (cas: 39489-79-7Recommanded Product: 5-Amino-2,4-dichlorophenol).

5-Amino-2,4-dichlorophenol (cas: 39489-79-7) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Recommanded Product: 5-Amino-2,4-dichlorophenol

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Transition-metal-free decarboxylative bromination of aromatic carboxylic acids was written by Quibell, Jacob M.;Perry, Gregory J. P.;Cannas, Diego M.;Larrosa, Igor. And the article was included in Chemical Science in 2018.Computed Properties of C8H7ClO3 This article mentions the following:

A transition metal-free decarboxylative bromination of aromatic acids was reported. The reaction is applicable to many electron-rich aromatic and heteroaromatic acids which have previously proved poor substrates for Hunsdiecker-type reactions. In addition, our preliminary mechanistic study suggested that radical intermediates are not involved in this reaction, which is in contrast to classical Hunsdiecker-type reactivity. Overall, the process demonstrates a useful method for producing valuable reagents from inexpensive and abundant starting materials. In the experiment, the researchers used many compounds, for example, 5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2Computed Properties of C8H7ClO3).

5-Chloro-2-methoxybenzoic acid (cas: 3438-16-2) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Computed Properties of C8H7ClO3

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors was written by Zhao, Bin;Li, Yixuan;Xu, Pan;Dai, Yang;Luo, Cheng;Sun, Yiming;Ai, Jing;Geng, Meiyu;Duan, Wenhu. And the article was included in ACS Medicinal Chemistry Letters in 2016.Computed Properties of C8H6ClFO2 This article mentions the following:

Fibroblast growth factor receptors (FGFRs) are important targets for cancer therapy. Herein, we describe the design, synthesis, and biol. evaluation of a novel series of 1H-pyrazolo[3,4-b]pyridine derivatives as potent and selective FGFR kinase inhibitors. On the basis of its excellent in vitro potency and favorable pharmacokinetic properties, compound I was selected for in vivo evaluation and showed significant antitumor activity in a FGFR1-driven H1581 xenograft model. These results indicated that I would be a promising candidate for further drug development. In the experiment, the researchers used many compounds, for example, Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3Computed Properties of C8H6ClFO2).

Methyl 2-chloro-4-fluorobenzoate (cas: 85953-29-3) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Computed Properties of C8H6ClFO2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

A Three-Component Approach to 3,5-Diaryl-1,2,4-thiadiazoles under Transition-Metal-Free Conditions was written by Xie, Hao;Cai, Jinhui;Wang, Zilong;Huang, Huawen;Deng, Guo-Jun. And the article was included in Organic Letters in 2016.Application In Synthesis of 2-Chloro-benzamidine hydrochloride This article mentions the following:

A novel route is disclosed for the synthesis of 1,2,4-thiadiazoles starting from amidines, elemental sulfur, and 2-methylquinolines or aldehydes under transition-metal-free conditions. This three-component approach affords efficient and rapid access to 3,5-diaryl substituted 1,2,4-thiadiazoles with good tolerance of a broad range of functional groups. Mechanistic studies reveal a radical-involved pathway. In the experiment, the researchers used many compounds, for example, 2-Chloro-benzamidine hydrochloride (cas: 18637-02-0Application In Synthesis of 2-Chloro-benzamidine hydrochloride).

2-Chloro-benzamidine hydrochloride (cas: 18637-02-0) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Application In Synthesis of 2-Chloro-benzamidine hydrochloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Role of the peri-effect in synthesis and reactivity of highly substituted naphthaldehydes: a novel backbone amide linker for solid-phase synthesis was written by Pittelkow, Michael;Boas, Ulrik;Jessing, Mikkel;Jensen, Knud J.;Christensen, Jorn B.. And the article was included in Organic & Biomolecular Chemistry in 2005.HPLC of Formula: 6834-42-0 This article mentions the following:

This work describes the design, synthesis and properties of a novel trialkoxynaphthalene-based backbone amide linker (NAL-3). The NAL-3 handle is based on a trialkoxynaphthaldehyde (NALdehyde-3) that was synthesized in nine high-yielding steps from 3-methoxyphenylacetic acid in 51% overall yield. The naphthalene ring system was constructed using a regioselective methanesulfonic acid-catalyzed ring-closing reaction. The tetra-substituted naphthalene derivative 1,3,6-trimethoxynaphthalene-2-carbaldehyde was selectively demethylated in the 1 position using BBr₃. The selectivity of this reaction is discussed, based on the crystal structures of above reactant and product, 1-hydroxy-3,6-dimethoxy-naphthalene-2-carbaldehyde, and in the context of the peri-effect. The new handle was anchored to an aminomethylated poly(styrene) solid support, followed by assembly of a model dipeptide, then a study of the cleavage properties under acidic conditions was carried out. Surprisingly, the trialkoxynaphthaldehyde-based handle proved less acid-labile than the dialkoxynaphthaldehyde handles, and this fact is discussed with respect to handle design. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0HPLC of Formula: 6834-42-0).

2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.HPLC of Formula: 6834-42-0

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Versatile Method for the Detection of Covalently Bound Substrates on Solid Supports by DART Mass Spectrometry was written by Sanchez, Laura M.;Curtis, Matthew E.;Bracamonte, Bianca E.;Kurita, Kenji L.;Navarro, Gabriel;Sparkman, O. David;Linington, Roger G.. And the article was included in Organic Letters in 2011.Product Details of 36157-41-2 This article mentions the following:

Anal. of substrates directly on solid phase resins without the need for sep. cleavage conditions remains an outstanding challenge in the field of solid phase synthesis. The authors now present the 1st example of simultaneous cleavage and mass spectrometric anal. of peptides from solid supports using direct anal. in real time (DART) mass spectrometry. This method is compatible with a diverse array of solid phase resins and is suitable for anal. of both peptides and organic substrates. In the experiment, the researchers used many compounds, for example, 2,5-Dichlorothiophene-3-carboxylic acid (cas: 36157-41-2Product Details of 36157-41-2).

2,5-Dichlorothiophene-3-carboxylic acid (cas: 36157-41-2) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Alkanes and aryl alkanes may be chlorinated under free radical conditions, with UV light. However, the extent of chlorination is difficult to control.Product Details of 36157-41-2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Palladium-Catalyzed Thiocarbonylation of Benzyl Chlorides with Sulfonyl Chlorides for the Synthesis of Arylacetyl Thioesters was written by Wang, Wei;Qi, Xinxin;Wu, Xiao-Feng. And the article was included in Advanced Synthesis & Catalysis in 2021.Name: 1-(Chloromethyl)-3-methylbenzene This article mentions the following:

A convenient procedure for the synthesis of thioesters RCH₂C(O)SR¹ (R = Ph, 3,4-dimethylphenyl, naphthalen-1-yl, thiophen-3-yl, etc.; R¹ = Ph, 2,4,6-trimethylphenyl, naphthalen-1-yl, etc.) has been developed via a palladium-catalyzed thiocarbonylation of benzyl chlorides RCH₂Cl with sulfonyl chlorides R¹S(O)₂Cl. Various arylacetyl thioesters were produced in good yields by using sulfonyl chlorides as an odorless sulfur source. Furthermore, W(CO)₆ exhibited dual roles as both a solid CO surrogate and reductant here. In the experiment, the researchers used many compounds, for example, 1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9Name: 1-(Chloromethyl)-3-methylbenzene).

1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances.While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available. Alkyl chlorides readily undergo attack by nucleophiles.Name: 1-(Chloromethyl)-3-methylbenzene

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Discovery of N-{1-[3-(3-Oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): An Allosteric Muscarinic M₁ Receptor Agonist with Unprecedented Selectivity and Procognitive Potential was written by Sams, Anette G.;Hentzer, Morten;Mikkelsen, Gitte K.;Larsen, Krestian;Bundgaard, Christoffer;Plath, Niels;Christoffersen, Claus T.;Bang-Andersen, Benny. And the article was included in Journal of Medicinal Chemistry in 2010.Electric Literature of C9H9ClO2 This article mentions the following:

The discovery and structure-activity relationship (SAR) of a series of allosteric muscarinic M₁ receptor agonists are described. Compound 17 (Lu AE51090) was identified as a representative compound from the series, based on its high selectivity as an agonist at the muscarinic M₁ receptor across a panel of muscarinic receptor subtypes. Furthermore, 17 displayed a high degree of selectivity when tested in a broad panel of G-protein-coupled receptors, ion channels, transporters, and enzymes, and 17 showed an acceptable pharmacokinetic profile and sufficient brain exposure in rodents in order to characterize the compound in vivo. Hence, in a rodent model of learning and memory, 17 reversed delay-induced natural forgetting, suggesting a procognitive potential of 17. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Electric Literature of C9H9ClO2).

2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Electric Literature of C9H9ClO2

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

De novo design, synthesis and pharmacological evaluation of new azaindole derivatives as dual inhibitors of Abl and Src kinases was written by Cheve, Gwenael;Bories, Cedric;Fauvel, Benedicte;Picot, Francois;Tible, Alix;Dayde-Cazals, Benedicte;Loget, Olivier;Yasri, Aziz. And the article was included in MedChemComm in 2012.Reference of 6834-42-0 This article mentions the following:

A fragment based drug design approach implemented in a MedChem-Decision platform led to the discovery of a series of 2,5-disubstituted 7-azaindole derivatives, e.g., I, as potent dual Abl and Src kinase inhibitors. Extensive structure-activity relationships and structure-based drug design studies guided the exploration of the specificity pocket within the active conformation of the ATP site of the two kinases. This led to the identification of a binding mode of the 7-azaindole core to the two kinases and the synthesis and pharmacol. evaluation of compounds that exhibit low nanomolar inhibition on both Abl and Src kinases. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Reference of 6834-42-0).

2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. The haloform reaction, using chlorine and sodium hydroxide, is also able to generate alkyl halides from methyl ketones, and related compounds. Chloroform was formerly produced thus.Reference of 6834-42-0

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics